Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. These include in vitro cell-kill models and cytostatic dye exclusion tests as well as in vivo measurement of tumor growth parameters in laboratory animals.
In vivo methods of screening investigative anticancer drugs, biologic response modifiers or radiotherapies. Human tumor tissue or cells are transplanted into mice or rats followed by tumor treatment regimens. A variety of outcomes are monitored to assess antitumor effectiveness.
Substances that inhibit or prevent the proliferation of NEOPLASMS.
A cell line derived from cultured tumor cells.
An experimental lymphocytic leukemia originally induced in DBA/2 mice by painting with methylcholanthrene.
Chemical substances, produced by microorganisms, inhibiting or preventing the proliferation of neoplasms.
Mutant mice homozygous for the recessive gene "nude" which fail to develop a thymus. They are useful in tumor studies and studies on immune responses.
Experimentally induced new abnormal growth of TISSUES in animals to provide models for studying human neoplasms.
Experimental transplantation of neoplasms in laboratory animals for research purposes.
Experimentally induced tumor that produces MELANIN in animals to provide a model for studying human MELANOMA.
Vaccines or candidate vaccines designed to prevent or treat cancer. Vaccines are produced using the patient's own whole tumor cells as the source of antigens, or using tumor-specific antigens, often recombinantly produced.
Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.
Manipulation of the host's immune system in treatment of disease. It includes both active and passive immunization as well as immunosuppressive therapy to prevent graft rejection.
Form of adoptive transfer where cells with antitumor activity are transferred to the tumor-bearing host in order to mediate tumor regression. The lymphoid cells commonly used are lymphokine-activated killer (LAK) cells and tumor-infiltrating lymphocytes (TIL). This is usually considered a form of passive immunotherapy. (From DeVita, et al., Cancer, 1993, pp.305-7, 314)
The action of a drug in promoting or enhancing the effectiveness of another drug.
Compounds with triple bonds to each side of a double bond. Many of these are CYTOTOXINS and are researched for use as CYTOTOXIC ANTIBIOTICS.
One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.
Mice homozygous for the mutant autosomal recessive gene "scid" which is located on the centromeric end of chromosome 16. These mice lack mature, functional lymphocytes and are thus highly susceptible to lethal opportunistic infections if not chronically treated with antibiotics. The lack of B- and T-cell immunity resembles severe combined immunodeficiency (SCID) syndrome in human infants. SCID mice are useful as animal models since they are receptive to implantation of a human immune system producing SCID-human (SCID-hu) hematochimeric mice.
All of the processes involved in increasing CELL NUMBER including CELL DIVISION.
Transplantation between animals of different species.
A carcinoma discovered by Dr. Margaret R. Lewis of the Wistar Institute in 1951. This tumor originated spontaneously as a carcinoma of the lung of a C57BL mouse. The tumor does not appear to be grossly hemorrhagic and the majority of the tumor tissue is a semifirm homogeneous mass. (From Cancer Chemother Rep 2 1972 Nov;(3)1:325) It is also called 3LL and LLC and is used as a transplantable malignancy.
Agents obtained from higher plants that have demonstrable cytostatic or antineoplastic activity.
Proteins, glycoprotein, or lipoprotein moieties on surfaces of tumor cells that are usually identified by monoclonal antibodies. Many of these are of either embryonic or viral origin.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Injections introduced directly into localized lesions.
Use of attenuated VIRUSES as ANTINEOPLASTIC AGENTS to selectively kill CANCER cells.
Techniques and strategies which include the use of coding sequences and other conventional or radical means to transform or modify cells for the purpose of treating or reversing disease conditions.
The phenomenon of target cell destruction by immunologically active effector cells. It may be brought about directly by sensitized T-lymphocytes or by lymphoid or myeloid "killer" cells, or it may be mediated by cytotoxic antibody, cytotoxic factor released by lymphoid cells, or complement.
Experimentally induced neoplasms of CONNECTIVE TISSUE in animals to provide a model for studying human SARCOMA.
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)
Antibodies produced by a single clone of cells.
Immunized T-lymphocytes which can directly destroy appropriate target cells. These cytotoxic lymphocytes may be generated in vitro in mixed lymphocyte cultures (MLC), in vivo during a graft-versus-host (GVH) reaction, or after immunization with an allograft, tumor cell or virally transformed or chemically modified target cell. The lytic phenomenon is sometimes referred to as cell-mediated lympholysis (CML). These CD8-positive cells are distinct from NATURAL KILLER CELLS and NATURAL KILLER T-CELLS. There are two effector phenotypes: TC1 and TC2.
The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability.
A sarcoma derived from deep fibrous tissue, characterized by bundles of immature proliferating fibroblasts with variable collagen formation, which tends to invade locally and metastasize by the bloodstream. (Stedman, 25th ed)
Tumors or cancer of the LUNG.
Tumor-selective, replication competent VIRUSES that have antineoplastic effects. This is achieved by producing cytotoxicity-enhancing proteins and/or eliciting an antitumor immune response. They are genetically engineered so that they can replicate in CANCER cells but not in normal cells, and are used in ONCOLYTIC VIROTHERAPY.
Tumors or cancer of the COLON.
A critical subpopulation of regulatory T-lymphocytes involved in MHC Class I-restricted interactions. They include both cytotoxic T-lymphocytes (T-LYMPHOCYTES, CYTOTOXIC) and CD8+ suppressor T-lymphocytes.
The total amount (cell number, weight, size or volume) of tumor cells or tissue in the body.
Agents and endogenous substances that antagonize or inhibit the development of new blood vessels.
Specialized cells of the hematopoietic system that have branch-like extensions. They are found throughout the lymphatic system, and in non-lymphoid tissues such as SKIN and the epithelia of the intestinal, respiratory, and reproductive tracts. They trap and process ANTIGENS, and present them to T-CELLS, thereby stimulating CELL-MEDIATED IMMUNITY. They are different from the non-hematopoietic FOLLICULAR DENDRITIC CELLS, which have a similar morphology and immune system function, but with respect to humoral immunity (ANTIBODY PRODUCTION).
Bone marrow-derived lymphocytes that possess cytotoxic properties, classically directed against transformed and virus-infected cells. Unlike T CELLS; and B CELLS; NK CELLS are not antigen specific. The cytotoxicity of natural killer cells is determined by the collective signaling of an array of inhibitory and stimulatory CELL SURFACE RECEPTORS. A subset of T-LYMPHOCYTES referred to as NATURAL KILLER T CELLS shares some of the properties of this cell type.
The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.
A family of non-enveloped viruses infecting mammals (MASTADENOVIRUS) and birds (AVIADENOVIRUS) or both (ATADENOVIRUS). Infections may be asymptomatic or result in a variety of diseases.
Antineoplastic antibiotic obtained from Streptomyces peucetius. It is a hydroxy derivative of DAUNORUBICIN.
The fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION.
Lymphocytes that show specificity for autologous tumor cells. Ex vivo isolation and culturing of TIL with interleukin-2, followed by reinfusion into the patient, is one form of adoptive immunotherapy of cancer.
Semisynthetic conjugates of various toxic molecules, including RADIOACTIVE ISOTOPES and bacterial or plant toxins, with specific immune substances such as IMMUNOGLOBULINS; MONOCLONAL ANTIBODIES; and ANTIGENS. The antitumor or antiviral immune substance carries the toxin to the tumor or infected cell where the toxin exerts its poisonous effect.
A pathologic process consisting of the proliferation of blood vessels in abnormal tissues or in abnormal positions.
DNA molecules capable of autonomous replication within a host cell and into which other DNA sequences can be inserted and thus amplified. Many are derived from PLASMIDS; BACTERIOPHAGES; or VIRUSES. They are used for transporting foreign genes into recipient cells. Genetic vectors possess a functional replicator site and contain GENETIC MARKERS to facilitate their selective recognition.
The use of two or more chemicals simultaneously or sequentially in the drug therapy of neoplasms. The drugs need not be in the same dosage form.
Experimentally induced mammary neoplasms in animals to provide a model for studying human BREAST NEOPLASMS.
Pyrido-CARBAZOLES originally discovered in the bark of OCHROSIA ELLIPTICA. They inhibit DNA and RNA synthesis and have immunosuppressive properties.
Technique using an instrument system for making, processing, and displaying one or more measurements on individual cells obtained from a cell suspension. Cells are usually stained with one or more fluorescent dyes specific to cell components of interest, e.g., DNA, and fluorescence of each cell is measured as it rapidly transverses the excitation beam (laser or mercury arc lamp). Fluorescence provides a quantitative measure of various biochemical and biophysical properties of the cell, as well as a basis for cell sorting. Other measurable optical parameters include light absorption and light scattering, the latter being applicable to the measurement of cell size, shape, density, granularity, and stain uptake.
A genus of bacteria that form a nonfragmented aerial mycelium. Many species have been identified with some being pathogenic. This genus is responsible for producing a majority of the ANTI-BACTERIAL AGENTS of practical value.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
The major interferon produced by mitogenically or antigenically stimulated LYMPHOCYTES. It is structurally different from TYPE I INTERFERON and its major activity is immunoregulation. It has been implicated in the expression of CLASS II HISTOCOMPATIBILITY ANTIGENS in cells that do not normally produce them, leading to AUTOIMMUNE DISEASES.
An inorganic and water-soluble platinum complex. After undergoing hydrolysis, it reacts with DNA to produce both intra and interstrand crosslinks. These crosslinks appear to impair replication and transcription of DNA. The cytotoxicity of cisplatin correlates with cellular arrest in the G2 phase of the cell cycle.
A soluble substance elaborated by antigen- or mitogen-stimulated T-LYMPHOCYTES which induces DNA synthesis in naive lymphocytes.
A transplantable, poorly differentiated malignant tumor which appeared originally as a spontaneous breast carcinoma in a mouse. It grows in both solid and ascitic forms.
A heterodimeric cytokine that plays a role in innate and adaptive immune responses. Interleukin-12 is a 70 kDa protein that is composed of covalently linked 40 kDa and 35 kDa subunits. It is produced by DENDRITIC CELLS; MACROPHAGES and a variety of other immune cells and plays a role in the stimulation of INTERFERON-GAMMA production by T-LYMPHOCYTES and NATURAL KILLER CELLS.
Lymphocytes responsible for cell-mediated immunity. Two types have been identified - cytotoxic (T-LYMPHOCYTES, CYTOTOXIC) and helper T-lymphocytes (T-LYMPHOCYTES, HELPER-INDUCER). They are formed when lymphocytes circulate through the THYMUS GLAND and differentiate to thymocytes. When exposed to an antigen, they divide rapidly and produce large numbers of new T cells sensitized to that antigen.
An alkaloid isolated from the stem wood of the Chinese tree, Camptotheca acuminata. This compound selectively inhibits the nuclear enzyme DNA TOPOISOMERASES, TYPE I. Several semisynthetic analogs of camptothecin have demonstrated antitumor activity.
A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
Polyacenes with four ortho-fused benzene rings in a straight linear arrangement. This group is best known for the subclass called TETRACYCLINES.
A class of drugs that differs from other alkylating agents used clinically in that they are monofunctional and thus unable to cross-link cellular macromolecules. Among their common properties are a requirement for metabolic activation to intermediates with antitumor efficacy and the presence in their chemical structures of N-methyl groups, that after metabolism, can covalently modify cellular DNA. The precise mechanisms by which each of these drugs acts to kill tumor cells are not completely understood. (From AMA, Drug Evaluations Annual, 1994, p2026)
Time schedule for administration of a drug in order to achieve optimum effectiveness and convenience.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
The treatment of a disease or condition by several different means simultaneously or sequentially. Chemoimmunotherapy, RADIOIMMUNOTHERAPY, chemoradiotherapy, cryochemotherapy, and SALVAGE THERAPY are seen most frequently, but their combinations with each other and surgery are also used.
The ability of tumors to evade destruction by the IMMUNE SYSTEM. Theories concerning possible mechanisms by which this takes place involve both cellular immunity (IMMUNITY, CELLULAR) and humoral immunity (ANTIBODY FORMATION), and also costimulatory pathways related to CD28 antigens (ANTIGENS, CD28) and CD80 antigens (ANTIGENS, CD80).
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
Agents that are capable of inserting themselves between the successive bases in DNA, thus kinking, uncoiling or otherwise deforming it and therefore preventing its proper functioning. They are used in the study of DNA.
An enediyne that alkylates DNA and RNA like MITOMYCIN does, so it is cytotoxic.
Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.
Resistance or diminished response of a neoplasm to an antineoplastic agent in humans, animals, or cell or tissue cultures.
Compounds that inhibit the activity of DNA TOPOISOMERASE I.
Morphologic alteration of small B LYMPHOCYTES or T LYMPHOCYTES in culture into large blast-like cells able to synthesize DNA and RNA and to divide mitotically. It is induced by INTERLEUKINS; MITOGENS such as PHYTOHEMAGGLUTININS, and by specific ANTIGENS. It may also occur in vivo as in GRAFT REJECTION.
An experimental lymphocytic leukemia of mice.
A cyclodecane isolated from the bark of the Pacific yew tree, TAXUS BREVIFOLIA. It stabilizes MICROTUBULES in their polymerized form leading to cell death.
Leukemia induced experimentally in animals by exposure to leukemogenic agents, such as VIRUSES; RADIATION; or by TRANSPLANTATION of leukemic tissues.
A tricyclic pentaglycosidic antibiotic from Streptomyces strains that inhibits RNA and protein synthesis by adhering to DNA. It is used as a fluorescent dye and as an antineoplastic agent, especially in bone and testicular tumors. Plicamycin is also used to reduce hypercalcemia, especially that due to malignancies.
Immunoglobulins induced by antigens specific for tumors other than the normally occurring HISTOCOMPATIBILITY ANTIGENS.
The complex series of phenomena, occurring between the end of one CELL DIVISION and the end of the next, by which cellular material is duplicated and then divided between two daughter cells. The cell cycle includes INTERPHASE, which includes G0 PHASE; G1 PHASE; S PHASE; and G2 PHASE, and CELL DIVISION PHASE.
Tumors or cancer of the human BREAST.
Substances that augment, stimulate, activate, potentiate, or modulate the immune response at either the cellular or humoral level. The classical agents (Freund's adjuvant, BCG, Corynebacterium parvum, et al.) contain bacterial antigens. Some are endogenous (e.g., histamine, interferon, transfer factor, tuftsin, interleukin-1). Their mode of action is either non-specific, resulting in increased immune responsiveness to a wide variety of antigens, or antigen-specific, i.e., affecting a restricted type of immune response to a narrow group of antigens. The therapeutic efficacy of many biological response modifiers is related to their antigen-specific immunoadjuvanticity.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Elements of limited time intervals, contributing to particular results or situations.
Agents that inhibit PROTEIN KINASES.
Active immunization where vaccine is administered for therapeutic or preventive purposes. This can include administration of immunopotentiating agents such as BCG vaccine and Corynebacterium parvum as well as biological response modifiers such as interferons, interleukins, and colony-stimulating factors in order to directly stimulate the immune system.
The phenomenon of antibody-mediated target cell destruction by non-sensitized effector cells. The identity of the target cell varies, but it must possess surface IMMUNOGLOBULIN G whose Fc portion is intact. The effector cell is a "killer" cell possessing Fc receptors. It may be a lymphocyte lacking conventional B- or T-cell markers, or a monocyte, macrophage, or polynuclear leukocyte, depending on the identity of the target cell. The reaction is complement-independent.
Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.
Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers.
A malignant epithelial tumor with a glandular organization.
Azoles of one NITROGEN and two double bonds that have aromatic chemical properties.
Glycosylated compounds in which there is an amino substituent on the glycoside. Some of them are clinically important ANTIBIOTICS.
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Acridines which are substituted in any position by one or more amino groups or substituted amino groups.
Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.
Human colonic ADENOCARCINOMA cells that are able to express differentiation features characteristic of mature intestinal cells such as the GOBLET CELLS.
Forceful administration into the peritoneal cavity of liquid medication, nutrient, or other fluid through a hollow needle piercing the abdominal wall.
Anaerobic degradation of GLUCOSE or other organic nutrients to gain energy in the form of ATP. End products vary depending on organisms, substrates, and enzymatic pathways. Common fermentation products include ETHANOL and LACTIC ACID.
Artificial, single or multilaminar vesicles (made from lecithins or other lipids) that are used for the delivery of a variety of biological molecules or molecular complexes to cells, for example, drug delivery and gene transfer. They are also used to study membranes and membrane proteins.
A critical subpopulation of T-lymphocytes involved in the induction of most immunological functions. The HIV virus has selective tropism for the T4 cell which expresses the CD4 phenotypic marker, a receptor for HIV. In fact, the key element in the profound immunosuppression seen in HIV infection is the depletion of this subset of T-lymphocytes.
Tumors or cancers of the KIDNEY.
Proteins prepared by recombinant DNA technology.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations, or by parent x offspring matings carried out with certain restrictions. All animals within an inbred strain trace back to a common ancestor in the twentieth generation.
A pyrimidine analog that is an antineoplastic antimetabolite. It interferes with DNA synthesis by blocking the THYMIDYLATE SYNTHETASE conversion of deoxyuridylic acid to thymidylic acid.
Precursor of an alkylating nitrogen mustard antineoplastic and immunosuppressive agent that must be activated in the LIVER to form the active aldophosphamide. It has been used in the treatment of LYMPHOMA and LEUKEMIA. Its side effect, ALOPECIA, has been used for defleecing sheep. Cyclophosphamide may also cause sterility, birth defects, mutations, and cancer.
Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.
An aminoacridine derivative that intercalates into DNA and is used as an antineoplastic agent.
Laboratory mice that have been produced from a genetically manipulated EGG or EMBRYO, MAMMALIAN.
CD4-positive T cells that inhibit immunopathology or autoimmune disease in vivo. They inhibit the immune response by influencing the activity of other cell types. Regulatory T-cells include naturally occurring CD4+CD25+ cells, IL-10 secreting Tr1 cells, and Th3 cells.
Systems for the delivery of drugs to target sites of pharmacological actions. Technologies employed include those concerning drug preparation, route of administration, site targeting, metabolism, and toxicity.
An encapsulated lymphatic organ through which venous blood filters.
Tumors or cancer of the PROSTATE.
Tumors or cancer of the LIVER.
A melanosome-associated protein that plays a role in the maturation of the MELANOSOME.
Angiostatic proteins that are formed from proteolytic cleavage of COLLAGEN TYPE XVIII.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control of gene action in neoplastic tissue.
Established cell cultures that have the potential to propagate indefinitely.
Compounds based on ANTHRACENES which contain two KETONES in any position. Substitutions can be in any position except on the ketone groups.
The giving of drugs, chemicals, or other substances by mouth.
The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.
A general term for various neoplastic diseases of the lymphoid tissue.
An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional ALKYLATING AGENTS causing cross-linking of DNA and inhibition of DNA synthesis.
A group of XANTHENES that contain a 9-keto OXYGEN.
A unifocal malignant tumor that consists of atypical pathological MAST CELLS without systemic involvement. It causes local destructive growth in organs other than in skin or bone marrow.
Compounds that inhibit the activity of DNA TOPOISOMERASE II. Included in this category are a variety of ANTINEOPLASTIC AGENTS which target the eukaryotic form of topoisomerase II and ANTIBACTERIAL AGENTS which target the prokaryotic form of topoisomerase II.
An ansa macrolide isolated from the MAYTENUS genus of East African shrubs.
Evaluation undertaken to assess the results or consequences of management and procedures used in combating disease in order to determine the efficacy, effectiveness, safety, and practicability of these interventions in individual cases or series.
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.
Antibodies from non-human species whose protein sequences have been modified to make them nearly identical with human antibodies. If the constant region and part of the variable region are replaced, they are called humanized. If only the constant region is modified they are called chimeric. INN names for humanized antibodies end in -zumab.
The dose amount of poisonous or toxic substance or dose of ionizing radiation required to kill 50% of the tested population.
A group of methylazirinopyrroloindolediones obtained from certain Streptomyces strains. They are very toxic antibiotics used as ANTINEOPLASTIC AGENTS in some solid tumors. PORFIROMYCIN and MITOMYCIN are the most useful members of the group.
The introduction of functional (usually cloned) GENES into cells. A variety of techniques and naturally occurring processes are used for the gene transfer such as cell hybridization, LIPOSOMES or microcell-mediated gene transfer, ELECTROPORATION, chromosome-mediated gene transfer, TRANSFECTION, and GENETIC TRANSDUCTION. Gene transfer may result in genetically transformed cells and individual organisms.
The highest dose of a biologically active agent given during a chronic study that will not reduce longevity from effects other than carcinogenicity. (from Lewis Dictionary of Toxicology, 1st ed)
A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.
The transfer of bacterial DNA by phages from an infected bacterium to another bacterium. This also refers to the transfer of genes into eukaryotic cells by viruses. This naturally occurring process is routinely employed as a GENE TRANSFER TECHNIQUE.
Benzene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.
A group of alkylating agents derived from mustard gas, with the sulfur replaced by nitrogen. They were formerly used as toxicants and vesicants, but now function as antineoplastic agents. These compounds are also powerful mutagens, teratogens, immunosuppressants, and carcinogens.
Antimetabolites that are useful in cancer chemotherapy.
Non-antibody proteins secreted by inflammatory leukocytes and some non-leukocytic cells, that act as intercellular mediators. They differ from classical hormones in that they are produced by a number of tissue or cell types rather than by specialized glands. They generally act locally in a paracrine or autocrine rather than endocrine manner.
A group of diterpenoid CYCLODECANES named for the taxanes that were discovered in the TAXUS tree. The action on MICROTUBULES has made some of them useful as ANTINEOPLASTIC AGENTS.
A costimulatory ligand expressed by ANTIGEN-PRESENTING CELLS that binds to CTLA-4 ANTIGEN with high specificity and to CD28 ANTIGEN with low specificity. The interaction of CD80 with CD28 ANTIGEN provides a costimulatory signal to T-LYMPHOCYTES, while its interaction with CTLA-4 ANTIGEN may play a role in inducing PERIPHERAL TOLERANCE.
Complex cytotoxic antibiotic obtained from Streptomyces flocculus or S. rufochronmogenus. It is used in advanced carcinoma and causes leukopenia.
Concentrated pharmaceutical preparations of plants obtained by removing active constituents with a suitable solvent, which is evaporated away, and adjusting the residue to a prescribed standard.
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
Experimentally induced tumors of the LIVER.
Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.
Manifestations of the immune response which are mediated by antigen-sensitized T-lymphocytes via lymphokines or direct cytotoxicity. This takes place in the absence of circulating antibody or where antibody plays a subordinate role.
Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).
Proteins whose abnormal expression (gain or loss) are associated with the development, growth, or progression of NEOPLASMS. Some neoplasm proteins are tumor antigens (ANTIGENS, NEOPLASM), i.e. they induce an immune reaction to their tumor. Many neoplasm proteins have been characterized and are used as tumor markers (BIOMARKERS, TUMOR) when they are detectable in cells and body fluids as monitors for the presence or growth of tumors. Abnormal expression of ONCOGENE PROTEINS is involved in neoplastic transformation, whereas the loss of expression of TUMOR SUPPRESSOR PROTEINS is involved with the loss of growth control and progression of the neoplasm.
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)
Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).
Glycoproteins found on the membrane or surface of cells.
Accumulation of a drug or chemical substance in various organs (including those not relevant to its pharmacologic or therapeutic action). This distribution depends on the blood flow or perfusion rate of the organ, the ability of the drug to penetrate organ membranes, tissue specificity, protein binding. The distribution is usually expressed as tissue to plasma ratios.
The milieu surrounding neoplasms consisting of cells, vessels, soluble factors, and molecules, that can influence and be influenced by, the neoplasm's growth.
A melanosome-specific protein that plays a role in the expression, stability, trafficking, and processing of GP100 MELANOMA ANTIGEN, which is critical to the formation of Stage II MELANOSOMES. The protein is used as an antigen marker for MELANOMA cells.
Inorganic or organic compounds that contain the basic structure RB(OH)2.
Organic compounds which contain platinum as an integral part of the molecule.
A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
A pyrano-acridone alkaloid found in RUTACEAE plants.
A cell surface protein-tyrosine kinase receptor that is overexpressed in a variety of ADENOCARCINOMAS. It has extensive homology to and heterodimerizes with the EGF RECEPTOR, the ERBB-3 RECEPTOR, and the ERBB-4 RECEPTOR. Activation of the erbB-2 receptor occurs through heterodimer formation with a ligand-bound erbB receptor family member.
Recombinant proteins produced by the GENETIC TRANSLATION of fused genes formed by the combination of NUCLEIC ACID REGULATORY SEQUENCES of one or more genes with the protein coding sequences of one or more genes.
A cytologic technique for measuring the functional capacity of tumor stem cells by assaying their activity. It is used primarily for the in vitro testing of antineoplastic agents.
Immunosuppression by reduction of circulating lymphocytes or by T-cell depletion of bone marrow. The former may be accomplished in vivo by thoracic duct drainage or administration of antilymphocyte serum. The latter is performed ex vivo on bone marrow before its transplantation.
Saturated azacyclopropane compounds. They include compounds with substitutions on CARBON or NITROGEN atoms.
A cell surface receptor involved in regulation of cell growth and differentiation. It is specific for EPIDERMAL GROWTH FACTOR and EGF-related peptides including TRANSFORMING GROWTH FACTOR ALPHA; AMPHIREGULIN; and HEPARIN-BINDING EGF-LIKE GROWTH FACTOR. The binding of ligand to the receptor causes activation of its intrinsic tyrosine kinase activity and rapid internalization of the receptor-ligand complex into the cell.
Compounds consisting of chains of AMINO ACIDS alternating with CARBOXYLIC ACIDS via ester and amide linkages. They are commonly cyclized.
Forceful administration under the skin of liquid medication, nutrient, or other fluid through a hollow needle piercing the skin.
An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I.
Compounds that include the amino-N-phenylamide structure.
Agents that interact with TUBULIN to inhibit or promote polymerization of MICROTUBULES.
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.
Cyclic esters of hydroxy carboxylic acids, containing a 1-oxacycloalkan-2-one structure. Large cyclic lactones of over a dozen atoms are MACROLIDES.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
Organic salts and esters of benzenesulfonic acid.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
The termination of the cell's ability to carry out vital functions such as metabolism, growth, reproduction, responsiveness, and adaptability.
Antibodies, often monoclonal, in which the two antigen-binding sites are specific for separate ANTIGENIC DETERMINANTS. They are artificial antibodies produced by chemical crosslinking, fusion of HYBRIDOMA cells, or by molecular genetic techniques. They function as the main mediators of targeted cellular cytotoxicity and have been shown to be efficient in the targeting of drugs, toxins, radiolabeled haptens, and effector cells to diseased tissue, primarily tumors.
Endogenous or exogenous substances which inhibit the normal growth of human and animal cells or micro-organisms, as distinguished from those affecting plant growth (= PLANT GROWTH REGULATORS).
Histochemical localization of immunoreactive substances using labeled antibodies as reagents.
Combinations of diagnostic or therapeutic substances linked with specific immune substances such as IMMUNOGLOBULINS; MONOCLONAL ANTIBODIES; or ANTIGENS. Often the diagnostic or therapeutic substance is a radionuclide. These conjugates are useful tools for specific targeting of DRUGS and RADIOISOTOPES in the CHEMOTHERAPY and RADIOIMMUNOTHERAPY of certain cancers.
Differentiation antigens residing on mammalian leukocytes. CD stands for cluster of differentiation, which refers to groups of monoclonal antibodies that show similar reactivity with certain subpopulations of antigens of a particular lineage or differentiation stage. The subpopulations of antigens are also known by the same CD designation.
Nonsusceptibility to the invasive or pathogenic effects of foreign microorganisms or to the toxic effect of antigenic substances.

A requirement for protein kinase C inhibition for calcium-triggered apoptosis in acute lymphoblastic leukemia cells. (1/3906)

We have evaluated the cytotoxicities of the combinations of calcium mobilizers and PKC inhibitors against human acute lymphoblastic leukemia (ALL) cells. Here we report that calcium mobilizers alone or PKC inhibitors alone do not induce apoptosis in human ALL cells. However, the combinations of calcium mobilizers with potent inhibitors of PKC cause significant apoptosis in ALL cells. Our results provide experimental evidence that PKC blocks Ca2+-triggered apoptosis in human ALL cells. Thus, PKC inhibitors can be used to enhance the antileukemic activity of chemical or biological agents that trigger an apoptotic calcium signal in ALL cells. The exquisite sensitivity of ALL cells to calcium-dependent apoptosis in the presence of PKC inhibitors could provide the basis for new treatment programs against ALL.  (+info)

Novel selective inhibitors for human topoisomerase I, BM2419-1 and -2 derived from saintopin. (2/3906)

Compounds BM2419-1 and -2 were isolated from a culture broth of a fungus Paecilomyces sp. BM2419. It was shown that these novel compounds were artifacts derived from saintopin, a dual inhibitor of topoisomerase I and II by independent processes. In the human topoisomerase I inhibition assay using the recombinant Saccharomyces cerevisiae, BM2419-1 and -2 inhibited selectively the yeast growth dependent on human topoisomerase I induction with IC50 values of 0.3 ng/ml and 6.0 ng/ml, respectively.  (+info)

Apicularens A and B, new cytostatic macrolides from Chondromyces species (myxobacteria): production, physico-chemical and biological properties. (3/3906)

A novel macrolide, apicularen A, was produced by several species of the genus Chondromyces. Initially it was discovered by bioassay-guided RP-HPLC-fractionation of culture extracts of Chondromyces robustus, strain Cm a13. Apicularen A showed no antimicrobial activity, but was highly cytotoxic for cultivated human and animal cells, with IC50 values ranging between 0.1 and 3 ng/ml. A cometabolite of apicularen A, the N-acetylglucosamine glycoside apicularen B, was distinctly less cytotoxic with IC50 values between 0.2 and 1.2 microg/ml, and showed weak activity against a few Gram-positive bacteria. Apicularen A is chemically closely related to the salicylihalamides A and B from the marine sponge Haliclona sp.  (+info)

BE-31405, a new antifungal antibiotic produced by Penicillium minioluteum. I. Description of producing organism, fermentation, isolation, physico-chemical and biological properties. (4/3906)

A new antifungal antibiotic, BE-31405, was isolated from the culture broth of a fungal strain, Penicillium minioluteum F31405. BE-31405 was isolated by adsorption on high porous polymer resin (Diaion HP-20), followed by solvent extraction, precipitation and crystallization. BE-31405 showed potent growth inhibitory activity against pathogenic fungal strains such as Candida albicans, Candida glabrata and Cryptococcus neoformans, but did not show cytotoxic activity against mammalian cells such as P388 mouse leukemia. The mechanism studies indicated that BE-31405 inhibited the protein synthesis of C. albicans but not of mammalian cells.  (+info)

Diperamycin, a new antimicrobial antibiotic produced by Streptomyces griseoaurantiacus MK393-AF2. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities. (5/3906)

Antibacterial antibiotics, diperamycin (1) was produced in the culture broth of Streptomyces griseoaurantiacus MK393-AF2. Various spectroscopic analyses of 1 suggested that 1 belonged to a member of cyclic hexadepsipeptide antibiotic. Antibiotic 1 had potent inhibitory activity against various Gram-positive bacteria including Enterococcus seriolicida and methicillin-resistant Staphylococcus aureus.  (+info)

Resveratrol suppresses cell transformation and induces apoptosis through a p53-dependent pathway. (6/3906)

Resveratrol, a plant constituent enriched in the skin of grapes, is one of the most promising agents for the prevention of cancer. However, the mechanism of the anti-carcinogenic activity of resveratrol is not well understood. Here we offer a possible explanation of its anti-cancer effect. Resveratrol suppresses tumor promoter-induced cell transformation and markedly induces apoptosis, transactivation of p53 activity and expression of p53 protein in the same cell line and at the same dosage. Also, resveratrol-induced apoptosis occurs only in cells expressing wild-type p53 (p53+/+), but not in p53-deficient (p53-/-) cells, while there is no difference in apoptosis induction between normal lymphoblasts and sphingomyelinase-deficient cell lines. These results demonstrate for the first time that resveratrol induces apoptosis through activation of p53 activity, suggesting that its anti-tumor activity may occur through the induction of apoptosis.  (+info)

Effect of retinoids on AOM-induced colon cancer in rats: modulation of cell proliferation, apoptosis and aberrant crypt foci. (7/3906)

We have previously reported that the retinoids, 4-(hydroxyphenyl)retinamide (4-HPR) and 9-cis-retinoic acid (RA) prevented azoxymethane (AOM)-induced colon tumors and along with 2-(carboxyphenyl)retinamide (2-CPR) prevented aberrant crypt foci (ACF). In this study, we evaluated the effect of 2-CPR on AOM-induced colon tumors and the effect of the three retinoids on apoptosis and cell proliferation. Male F344 rats were administrated 15 mg/kg AOM at weeks 7 and 8 of age. 2-CPR (315 mg/kg) was administered in the diet starting either 1 week before or at week 12 after the first dose of AOM. The rats continued to receive the 2-CPR until killed at week 46. Unlike the demonstrated prevention of colon cancer by the other two retinoids, both dosing schedules of 2-CPR resulted in an approximate doubling of the yield of colon tumors. In adenomas, 2-CPR, 4-HPR and 9-cis-RA were equally effective in reducing mitotic activity, while only 4-HPR and 9-cis-RA but not 2-CPR enhanced apoptosis. When administered for only the 6 days prior to killing 4-HPR but not 2-CPR decreased the Mitotic Index and increased the Apoptotic Index in adenomas. In non-involved crypts, chronic exposure to 4-HPR and 9-cis-RA in contrast to 2-CPR reduced the Mitotic Index and enhanced the Apoptotic Index. In concurrence with our previous study, both 2-CPR and 4-HPR were very potent in preventing ACF when administered in the diet starting 1 week before the first dose of AOM and continuing for the 5 weeks of the study. Hence, unlike the other two retinoids, 2-CPR, although very potent in preventing ACF, enhanced rather than prevented AOM-induced colon cancer. Furthermore, our results suggest that the effect of 2-CPR on tumor yield is different from 4-HPR and 9-cis-RA because, unlike them, it does not enhance apoptosis.  (+info)

Synthesis, anti-HIV and anticancer activities of new 4-(2-mercaptobenzenesulfonyl)perhydro-1,2,4-triazin-3-ones. (8/3906)

Syntheses of N-(6-chloro-1,1-dioxo-7-R1-1,4,2-benzodithiazyn-3-yl)-N'-(2- hydroxyethyl)hydrazines (IIa-d], N-(6-chloro-1,1-dioxo-7-methyl-1,4,2-benzodithiazyn-3-yl)-N'-(2- chloroethyl)hydrazine [IV], 4-(4-chloro-5-R1-2-mercaptobenzenesulfonyl)perhydro-1,2,4-triaz in-3-ones [IIIa-d] and 5-chloro-4-methyl-2-(3-oxoperhydro-1,2,4-triazin-4- ylsulfonyl)phenylthioacetic acid [V] have been described. Preliminary screening data have indicated that compounds [IIIa-d] exhibit either a moderate or a high anti-HIV activity and a moderate anticancer activity in some human tumor cell lines.  (+info)

BioAssay record AID 212 submitted by DTP/NCI: NCI In Vivo Anticancer Drug Screen. Data for tumor model Colon Carcinoma 38 (subcutaneous) in B6D2F1 (BDF1) mice.
BioAssay record AID 282 submitted by DTP/NCI: NCI In Vivo Anticancer Drug Screen. Data for tumor model L1210 Leukemia resistant to A Terephthalanilide; NSC 38280 (intraperitoneal) in B6D2F1 (BDF1) mice.
D. THE BIOCHEMICAL PATHWAYS OF PYRIMIDINE AND PURINE SYNTHESIS AS TARGETS OF COMBINATION CHEMOTHERAPY WITH NEW ANTICANCER AGENTS. Investigation of the possibilities of blocking simultaneously several biochemical pathways leading to the synthesis of pyrimidine and purine nucleotides. Combinations of recently developed compounds, which show remarkable activity against enzymes involved in the de novo synthesis of pyrimidine nucleotides will be used for this purpose. A series of established and primary human cancer cell lines will be used in the in vitro chemosensitivity assays for these combinations. The results are expected to identify new targeting methodologies against cancer, which may then be directly applicable in the chemotherapeutic treatment of cancer patients.. ...
The project aims to develop high-content, multiplex assays capable of simultaneously detecting 35 National Institute of Allergy and Infectious Diseases category A, B, and C viral agents, plus quantifying cytokine and chemokine responses in patients.. ...
These results indicate that PSK has cytotoxic activity in vitro on tumor cell lines. This new cytotoxic activity of PSK on tumour cells is independent of its
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
Doctors have a new ally to deal with cases of cancer patients who have two or more possible treatments: the chemosensitivity test.
In Vitro Chemoresponse in Metachronous Pairs of Ovarian Cancers, H. J. Dalton, J. V. Fiorica, R. P. Rocconi, F. O. Recio, J. L. Lovecchio, M. O. Burrell, E. C. Grendys, D. K. Wang, T. H. Wang, B. J. Monk, and +3 additional authors. ...
Learn Cancer Agents for DA final facts using a simple interactive process (flashcard, matching, or multiple choice). Finally a format that helps you memorize and understand. Browse or search in thousands of pages or create your own page using a simple wizard. No signup required!
TY - JOUR. T1 - Adenosine triphosphate-based chemotherapy response assay predicts long-Term survival of primary epithelial ovarian cancer. AU - Li, Lan Ying. AU - Kim, Sang Wun. AU - Nam, Eun Ji. AU - Lee, Jungyun. AU - Kim, Sunghoon. AU - Kim, Young Tae. PY - 2019/2/1. Y1 - 2019/2/1. N2 - Objective The aim of this study is to analyze the long-Term relapse-free survival and overall survival outcomes of primary ovarian cancer patients using adenosine triphosphate-based chemotherapy response analysis. Methods In total, 162 primary epithelial ovarian cancer patients who underwent chemotherapy response assay for carboplatin, cisplatin, and paclitaxel by adenosine triphosphate-based chemotherapy response analysis prior to chemotherapy between December 2006 and November 2016 were retrospectively reviewed. Chemosensitivity with single or combined three agents and clinical characteristics of patients were studied to understand their correlation with long-Term relapse-free survival and overall survival. ...
The present study aims to investigate the anti-proliferative, apoptotic properties of prodigiosin, using a human oral squamous cell carcinoma HSC-2 cell line as a model system. HSC- 2 cells were cultured in the presence of prodigiosin at various concentrations (1-30µg/ml) for 48 h and the percentage of cell viability was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. The results showed that prodigiosin inhibited the cells viability in time and concentration dependent characteristics at different concentrations. We found that anti-proliferative effect of prodigiosin was associated with apoptosis on HSC-2 cells by determinations of DNA fragmentation, Hoechst 33258 staining, caspases activity, and TNF-α was significantly changed when compare DMSO control group. In addition, activity of lactate dehydrogenase (LDH) release increased when the cells incubated with prodigiosin at various concentrations and times. These results suggested that prodigiosin ...
NSC 652287 is a representative of a novel class of thiophene derivatives discovered in the NCI Anticancer Drug Screen for their activity against the subpanel of cell lines derived from renal cancer, a disease for which present chemotherapy has limited activity. The present study shows that thiophene NSC 652287 is a potent inducer of apoptosis at submicromolar concentrations. Apoptosis was associated with p53 elevation and decrease of p21WAF1 protein levels in A498 cells. By contrast, lower NSC 652287 concentrations induced elevation of both p53 and p21WAF1 and cell cycle arrest (Fig. 3 and Table 2). A decrease of p21WAF1 in spite of p53 elevation at NSC 652287 concentrations that induced apoptosis was probably due to p21WAF1 degradation during apoptosis. p21WAF1 is indeed a substrate for caspases (Gervais et al., 1998).. Although A498 cells have wild-type p53 and are very sensitive to NSC 652287, two of the most resistant kidney cell lines of the NCI Anticancer Drug Screen, ACHN and UO-31, also ...
Creative Biogene has developed several approaches to investigate zebrafish visual function, including optomotor response (OMR) assay, optokinetic response assay, escape response, startle response, and visual motor response assay.
TY - JOUR. T1 - Design, synthesis and potent cytotoxic activity of novel 7-(N-[(substituted-sulfonyl)piperazinyl]-methyl)-camptothecin derivatives. AU - Zhu,Gao Xiang. AU - Cheng,Pi Le. AU - Goto,Masuo. AU - Zhang,Na. AU - Morris-Natschke,Susan L.. AU - Hsieh,Kan Yen. AU - Yang,Guan Zhou. AU - Yang,Qian Ru. AU - Liu,Ying Qian. AU - Chen,Hai Le. AU - Zhang,Xiao Shuai. AU - Lee,Kuo Hsiung. PY - 2017. Y1 - 2017. N2 - In an effort to discover potent camptothecin-derived antitumor agents, novel camptothecin analogues with sulfonylpiperazinyl motifs at position-7 were designed and synthesized. They were evaluated for in vitro cytotoxicity with the sulforhodamine-B (SRB) method in five types of human tumor cell lines, A-549, MDA-MB-231, KB, KB-VIN and MCF-7. With IC50 values in the low μM to nM level, most of the new analogues showed greater cytotoxicity activity than the reference compounds irinotecan and topotecan. Furthermore, compounds 12l (IC50, 1.2 nM) and 12k (IC50, 20.2 nM) displayed the ...
Triazolyl RuII, RhIII, OsII, and IrIII Complexes as Potential Anticancer Agents: Synthesis, Structure Elucidation, Cytotoxicity, and DNA Model Interaction Studies. Organometallics, 2019
Background: Zinc has important effects on the human health, especially on the structural and functional activities of immune system. This study was carried out to examine the in vitro cytotoxic effects of Zinc on the Raji cell line. Materials and methods: The cell line was exposed to different concentrations of ...
9 Panel Urine Drug Screens are available at AMH Nationwide. Call us at ☎ (888) 493-2521 to find more information about a lab near you!
Hi, I am trying to find the correct code for Medicare and Medicaid to be used for drug screens. We currently have our CLIA waiver and have been using
1 Answer - Posted in: klonopin, xanax, prescription, drug screen, drug - Answer: Most likely yes. It depends on the test as to how they show but you ...
A wide variety of research has shown that γ-tubulin activates during cell division and that it is overexpressed in a portion of cancer cells, so it holds potential as a target protein for new anticancer agents with few side effects. Despite this research, no specific inhibitors have thus far been discovered.
Inhibition of tubulin polymerization has been identified as a significant characteristic of potential anticancer agents. Tubulin is a heterodimeric protein of a and b polypepetide chains, each with a molecular weight of ...
Kinase Panel (For detailed kinase panel list, please click here). Cell Line Panel. GPCRs (For detailed GPCR assay list, please click here). Radioactive Assays. Key equipment & software supporting in vitro screening. ...
Merrimack Pharmaceuticals is combining biology, computing, and engineering in order to gain a comprehensive understanding of the dynamics of different types of cancer and then use that information to develop new therapeutics.
Sigma-Aldrich offers abstracts and full-text articles by [Jie Yang, Guo-Yun Liu, Fang Dai, Xiao-Yan Cao, Yan-Fei Kang, Li-Mei Hu, Jiang-Jiang Tang, Xiu-Zhuang Li, Yan Li, Xiao-Ling Jin, Bo Zhou].
These easy to use, on-site drugs of abuse screen combines a collection cup and testing device that delivers instant results, convenience, and accuracy within minutes.
LabCorp Blood Diagnostic Test - M-F 7:30AM-12:00N M-F 1:00PM-4:30PM LUNCH 12:00N-1:00PM DRUG SCREENS 7:30AM-11:00A DRUG SCREENS 1:00PM-4:00PM
I have heard of cancer agents being used to help with sign and symptoms of CIPD. Exactly which agents are used and at what dose/frequency. What is their proposed mechanism of action? Also how is meth...
But this patch is exactly what has been included in AUCTeX 11.90.2 3 , months ago. So what you actually want to suggest is to make a true , release out of 11.90.2, dont you? Not necessarily. 11.90 + this one line patch is different from 11.90.2 ;-) Norbert -- PREINING Norbert Accelia Inc. + JAIST + TeX Live + Debian Developer GPG: 0x860CDC13 fp: F7D8 A928 26E3 16A1 9FA0 ACF0 6CAC A448 860C DC13 ...
M-F 6:30 AM-11:30 AM & 12:30 PM-3:00 PM,SA 7:00 AM-11:00 AM; DRUG SCREEN: M-F 6:30 AM-11:30 AM & 12:30 PM-2:30 PM,SA 7:00 AM-10:30 ...
Clinical Application of the Adenosine Triphosphate-based Response Assay in Intravesical Chemotherapy for Superficial Bladder Cancer Adenosine triphosphate;chemotherapy response assay;superficial bladder cancer; Objective: To investigate correlations between adenosine triphosphate chemotherapy response assay (ATP-CRA) and clinical outcomes after ATP-CRA-based chemotherapy for drug selection in patients receiving intravesical chemotherapy to prevent recurrence of superficial bladder cancer after surgery. Methods: The chemosensitivities of 12 anticancer drugs were evaluated, including 5-Fu ADM, and EPI, using ATP-CRA and primary tumor cell culture in 54 patients. In addition, a further 58 patients were treated according to clinical experience. Differences in post-chemotherapeutical effects between drug sensitivity assay and experience groups were compared. Results: The evaluable rate of the test was 96.3%, the clinical effective rate was 80.8%, the sensitivity rate was 97.6% (41/42), the specificity was
The evolution of strategies at the National Cancer Institute (NCI) illustrates the changes in screening that have resulted from advances in cancer biology. The Developmental Therapeutics Program (DTP) operates a tiered anti-cancer compound screening program with the goal of identifying novel chemical leads and biological mechanisms. The DTP screen is a three phase screen which includes: an initial screen which first involves a single dose cytotoxicity screen with the 60 cell line assay. Those passing certain thresholds are subjected to a 5 dose screen of the same 60 cell-line panel to determine a more detailed picture of the biological activity. A second phase screen establishes the maximum tolerable dosage and involves in vivo examination of tumor regression using the hollow fiber assay. The third phase of the study is the human tumor xenograft evaluation. Active compounds are selected for testing based on several criteria: disease type specificity in the in vitro assay, unique structure, ...
Cancer is one of the leading causes of death worldwide. According to the WHO, cancer accounted for 7.4 million deaths world wide in 2004. The metallo-compound cisplatin has been used for years as an effective antitumor agent for treating solid tumours such as breast, bladder, lung, oesophageal, and head and neck carcinomas. However, the use of cisplatin as an antitumor agent has been limited because of its association with problems such as lack of selectivity for cancer cells over normal cells, development of resistance to cisplatin treatment, and side effects such as nephrotoxicity. Recent studies on anticancer drugs have focussed on alternative anticancer agents such as gold compounds in both Au(I) and (III) oxidation states, which have shown to be potential anticancer drug agents because of their ability to induce apoptosis in several human cancer cells. Some gold complexes have shown to be able to selectively kill cancer cells over normal cells ...
Simvastatin and lovastatin are statins traditionally used for lowering serum cholesterol levels. However, there exists evidence indicating their potential chemotherapeutic characteristics in cancer. In this study, we used bioinformatic analysis of publicly available data in order to systematically identify the genes involved in resistance to cytotoxic effects of these two drugs in the NCI60 cell line panel. We used the pharmacological data available for all the NCI60 cell lines to classify simvastatin or lovastatin resistant and sensitive cell lines, respectively. Next, we performed whole-genome single marker case-control association tests for the lovastatin and simvastatin resistant and sensitive cells using their publicly available Affymetrix 125K SNP genomic data. The results were then evaluated using RNAi methodology. After correction of the p-values for multiple testing using False Discovery Rate, our results identified three genes (NRP1, COL13A1, MRPS31) and six genes (EAF2, ANK2, AKAP7, STEAP2,
In the present study, investigations were carried out to screen the anticancer activities of fenugreek seedoil against cancer cell lines (HEp-2, MCF-7, WISH cells), and a normal cell line (Vero cells). Cytotoxicity wasassessed with MTT and NRU assays, and cellular morphological alterations were studied using phase contrastlight microscopy. All cells were exposed toi 10-1000 μg/ml of fenugreek seed oil for 24 h. The results show thatfenugreek seed oil significantly reduced the cell viability, and altered the cellular morphology in a dose dependentmanner. Among the cell lines, HEp-2 cells showed the highest decrease in cell viability, followed by MCF-7, WISH,and Vero cells by MTT and NRU assays. Cell viability at 1000 μg/ml was recorded as 55% in HEp-2 cells, 67%in MCF-7 cells, 75% in WISH cells, and 86% in Vero cells. The present study provides preliminary screeningdata for fenugreek seed oil pointing to potent cytotoxicity against cancer cells.
R)- and (S)-Goniothalamin (1) and analogues 2-9 were efficiently prepared in high overall yield and enantiomeric purity, and their cytotoxic activities were evaluated against eight human cancer cell lines. A structure-activity relationship study (SAR) allowed us to establish the relevant structural features for the cytotoxic activity of goniothalamin analogues. In addition, we have identified non-natural form of goniothalamin (S)-1 and analogue 5 as the highest and more selective cytotoxic compounds against kidney cancer cell growth (786-0) with IC50 = 4 and 5 nM, respectively, and compound 8 (IC50 = 4 nM) as the more potent against breast cancer cells with resistance phenotype for adryamycin (c) 2005 Elsevier Ltd. All rights reserved ...
Indicated groups were compared using Wilcoxon matched\pairs signed rank test (****DH10b (Invitrogen) were transformed with 3?L of the reaction product via heat shock at 42C for 45?s and plated onto 100?g/mL ampicillin containing LB Broth with agar (Sigma) plates. 3, = 115258C6762C7645C60T follicular helper, LNsCD4+CD44+CD62Llow CXCR5+PD\1+ 3, = 345658C6762C7645C60T regulatory, Continue Reading. ...
This study addresses three important issues regarding CD/5-FC VDEPT. First, data presented in Figs. 1 ⇓ and 3 ⇓ demonstrate that cell lines derived from both GI and non-GI tumors display similar in vitro sensitivity to both 5-FU and AdCMVCD/5-FC on continuous 5-day drug exposure using the 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium assay of cellular respiration. Nonparametric analysis of median 5-FU (Fig. 1) ⇓ and AdCMVCD/5-FC (Fig. 3) ⇓ sensitivity (IC50) of 14 tumor cell lines (2 colon, 5 pancreatic, 4 glioma, and 3 prostatic cell lines) revealed no significant differences among the four tumor cell types tested (P = 0.1 and 0.24, respectively). A similar analysis was performed on publicly available 5-FU toxicity data from the National Cancer Institute Developmental Therapeutics Program Disease-oriented Anticancer Drug Screen (28) . The National Cancer Institute screens approximately 10,000 compounds/year using a sulforhodamine B protein ...
The present work describes the preparation of three novel series of compounds based on the structure of goniothalamin, a natural styryl lactone which has been found to display cytotoxic and antiproliferative activities against a variety of cancer cell lines. A focused library of 29 novel goniothalamin analogues was prepared and evaluated against seven human cancer cell lines. While the gamma-pyrones and the azagoniothalamin analogues were less potent than the lead compound, 2,4-dimethoxy analogue 88 has shown to be more potent in vitro than goniothalamin against all cancer cell lines evaluated. Furthermore, it was more potent than doxorubicin against NCI-ADR/RES, OVCAR-03 and HT-29 while being less toxic to human keratinocytes (HaCat). The 3,5-dimethoxy analogue 90 and 2,4,5-trimethoxy analogue 92 also displayed promising antiproliferative activity when compared to goniothalamin ( 1). These results provide new elements for the design and synthesis of novel representatives of this family of ...
In this study, the relationships between the chemical structure and cytotoxic activity of betulinic acid (1) derivatives were investigated. Eight lupane derivatives (1-8), one of them new (6), five diosphenols (9-13), four of them new (10-13), two new norderivatives (14 and 15), five seco derivatives (16-20), four of them new (16, 17, 19, and 20), and three new seco-anhydrides (21-23) were synthesized from 1, and their activities were compared with the activities of known compounds. The effects of substitution on the A-ring and esterification of the carboxyl group in position 28 on cytotoxicity were of special interest. Significant cytotoxic activity against the T-lymphoblastic leukemia cell line CEM was found in diosphenols 9 and 13 (TCS(50) 4 and 5 micromol/L) and seco-anhydrides 22 and 23 (TCS(50) 7 and 6 micromol/L). All compounds were also tested on cancer cell lines HT 29, K562, K562 Tax, and PC-3, and these confirmed activity of diosphenols 9, 10, and 11 and anhydride 22. Diosphenols, as ...
This study presents the synthesis of nineteen 1-(substitutedbenzoyl)-4- benzhydrylpiperazine and 1-[(substitutedphenyl)sulfonyl]-4-benzhydrylpiperazine derivatives. In vitro cytotoxic activities of the compounds were screened against hepatocellular (HUH-7), breast (MCF-7) and colorectal (HCT-116) cancer cell lines by sulphorhodamine B assay. Among the test compounds, benzamide derivatives had high cytotoxic activity whereas sulfonamide derivatives showed variable 50% growth inhibition (GI50). © Georg Thieme Verlag KG Stuttgart · New York ...
Encodes a MAP kinase protein. MPK12 interacts with the IBR5 protein phosphatase in vitro and in vivo, and it can be dephosphorylated and inactivated by IBR5. MPK12 appears to be a negative regulator of auxin signlaing. MPK12 RNAi lines are hypersensitive to auxin in root elongation and transcriptional response assays, but they appear to have normal sensitivity to ABA. MPK12 is a nuclear protein and its kinase activity is increased following auxin treatment. MPK12 transcripts are widely expressed in seedlings, but MPK12 expression is stronger in guard cells than in other cell types in m [...] (372 aa ...
The current scale of cancer diseases resembles an epidemic: annually, over seven million people worldwide die of malignant tumors and about ten million new cancer cases are diagnosed. Although many cancer types are successfully treated, the consequences of such a treatment are frequently no less injurious than the illness itself. It is no wonder that researchers are constantly searching for and designing new, more efficient, and, which is of the paramount importance, safer therapies and drugs. Note here that the substances displaying an anticancer activity are detectable in most unlikely places such as breast milk…
ChemPartner is a leading research organization providing high-quality and cost-effective services for the pharmaceutical and biotechnology industry ...
Rapid results for the ED. Accuracy for the lab. Alere Triage® TOX Delivers. When choosing a rapid drug screen there are many factors to consider: accuracy, ease-of-use, system interface capabilities and test selectivity. The instrumentation of the Alere Triage® TOX Drug Screen platform provides these features.
New series of 6-(arylthio)uracils, 6-(4-substituted-1-piperazinyl)uracils, 2,4,5-trioxo-1H,3H-benzothiopyrano[2,3-d]pyrimidine and 5-aryl-2,4-dioxo-1H,3H-pyrimido[5,4-f]benzo[1,4]thiazepines have been prepared and screened for their in vitro activity against herpes simplex-1 virus (HSV-1) and human immunodeficiency virus-1 (HIV-1). The in vitro cytotoxic activity was also evaluated. The results of biological testing revealed that compound 5b showed marginal activity against HSV-1, while compounds 5b and 5f exhibited marginal activity against HIV-1. The rest of the tested compounds were found devoid of antiviral activity against both HSV-1 and HIV-1 ...
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Pdf is an enzyme that, during protein production, removes a modification called an N-formyl group from the first amino acid, a methionine, in the protein chain. While work began on the development of antibiotics against what was thought to be a bacterial-exclusive enzyme, genome-based data searches identified several classes of Pdf-like sequences in parasites, plants and mammals. Subsequent studies showed that the Pdfs were active both in culture and in the living organism, thus potentially derailing the usefulness of these antibiotics for specifically combating infectious agents. In previous studies, Scheinberg and colleagues had found that actinonin had an antiproliferative effect on human cancer cell lines and on tumor growth in a mouse model. They theorized this growth inhibitory activity might be related to actinonin s inhibition of human Pdf ...
Selective cytotoxicity of oxysterols through structural modulation on rings A and B. Synthesis, in vitro evaluation, and SAR.: Chemically diverse oxysterols wer
2-(4-hydroxyphenyl)-4-(1-(4-hydroxyphenyl)methylidene)-5-oxotetrahydro-3-furancarboxylic acid: cytotoxic constituent of roots of Chaerophyllum hirsutum; structure in first source
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ATCC has developed two brain cancer cell line panels with varying degrees of genetic complexity, including mutations in TP53 and PTEN.
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Ropathy can be a novel technique in modern medicine. The relevance of NFB signaling in most cancers progression is further verified with the proven fact that this signaling pathway is most likely essentially the most studied pathway when it comes to assessing the action of potential anticancer agents. Normally, here is the really 1st pathway evaluated. To be a consequence, nearly every one nutraceutical is documented to inhibit the NFB signaling pathway to some extent. Especially, theres mind-boggling information supporting the inhibition of NFB signaling by curcumin [869], which almost makes it seem as though curcumin is often a certain inhibitor of NFB signaling; even so, the good thing about curcumin is proscribed thanks, in part, for its bad systemic and focus on tissueNutrients 2015,bioavailability. As Pub Releases ID: reviewed higher than, curcumin failed in translational experiments due to the fact of its lousy ...
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Tens of thousands have come to eastern Madagascar seeking the precious gem in the past six months, disfiguring a protected environmental area and prompting calls for military intervention.
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Kibdelone B is a minor analogue of a potent antitumor complex isolated from Kibdelosporangium sp.. Structurally, kibdelone B is related to lysolipin and albofungin, however no comparative investigation of this class has been reported ...
... drug screening assays, antitumor MeSH E05.337.550.200.800 - tumor stem cell assay MeSH E05.337.550.200.900 - xenograft model ... drug screening assays, antitumor MeSH E05.200.500.388.930 - tumor stem cell assay MeSH E05.200.500.410 - electroporation MeSH ... multiphasic screening MeSH E05.318.308.250.580.580 - neonatal screening MeSH E05.318.308.250.580.925 - vision screening MeSH ... antitumor assays MeSH E05.337.550.200.900.830 - subrenal capsule assay MeSH E05.337.550.400 - microbial sensitivity tests MeSH ...
"Performance of Interferon-Gamma Release Assays for Tuberculosis Screening in Pediatric Inflammatory Bowel Disease". Journal of ... "U.S. Food and Drug Administration (FDA) (Press release). 30 May 2018. Retrieved 31 May 2018.. ... "A Prospective Study to Monitor for Tuberculosis During Anti-tumour Necrosis Factor Therapy in Patients With Inflammatory Bowel ... A series of drugs in development looks to disrupt the inflammation process by selectively targeting an ion channel in the ...
Using a line of CD4+ T cells that they had made, they developed an assay to screen drugs for their ability to protect CD4+ T ... leading to the development of the antitumor agent 6-mercaptopurine. Jerome Horwitz of the Barbara Ann Karmanos Cancer Institute ... another drug that had shown effective anti-HIV activity in the laboratory. This initial trial of AZT proved that the drug could ... This assay could simultaneously test both the anti-HIV effect of the compounds and their toxicity against infected T cells. In ...
Studies related to antitumor antibiotics. Part V. Reactions of mitomycin C with DNA examined by ethidium fluorescence assay. ... Microbial drug discovery: 80 years of progress. J Antibiot. 62:5-16. Lown JW, Begetter A, Johnson D, Morgan AR. 1976. ... Research on Antibiotic Screening in Japan over the Last Decade: A Producing Microorganisms Approach. Actinomycetologica. 9:100- ... Many natural compounds have led to the discovery of drugs used to treat human disease. Out of the 22,500 biologically active ...
It enhances antitumor activity of some other drugs such as vincristine. Dactolisib seems to inhibit effectively both wild-type ... New mTOR-specific inhibitors came forth from screening and drug discovery efforts. These compounds block activity of both mTOR ... Thus, this data is based on preclinical assays, based on in vitro cultured tumor cell lines, which suggest that the effects of ... Compared with drugs that inhibit either mTORC1 or PI3K, these drugs have the benefit of inhibiting mTORC1, mTORC2, and all the ...
It enhances antitumor activity of some other drugs such as vincristine.[20] Dactolisib seems to inhibit effectively both wild- ... New mTOR-specific inhibitors came forth from screening and drug discovery efforts. These compounds block activity of both mTOR ... this data is based on preclinical assays, based on in vitro cultured tumor cell lines, which suggest that the effects of mTOR ... Temsirolimus is pro-drug of rapamycin. It is approved by the U.S. Food and Drug Administration (FDA)[25] and the European ...
Applying the revised screen led to the discovery of the potent biological activity of ciclosporin on 31 January 1972. This drug ... Guided by Stähelin's in-vitro and in-vivo assays, they found the active compound responsible for the good antitumor activity of ... Stähelin's invention of this procedure initiated an innovative screening system for discovering immunosuppressant drugs lacking ... This screening process was first used in the pharmacology department in January 1970, before Jean F. Borel joined Stähelin's ...
Also, amanitin-based antibody-drug conjugates using an anti-Her2 antibody such as trastuzumab showed high antitumor activity in ... Urine screening is generally most useful within 48 hours of ingestion. Treatment is mainly supportive (gastric lavage, ... As early as the 1980s, antibody-based assays (immunoassays) were developed for amanitin (but more often recognize amatoxins as ... "What are antibody-drug conjugates?". ADC Review / Journal of Antibody-drug Conjugates. ISSN 2327-0152. Retrieved 26 May 2017. ...
Tetramer assays are used for single-cell phenotyping and cell counting, and offer an important advantage over other methods, ... MHC tetramers are used in studies of pathogen immunity and vaccine development, in evaluation of antitumor responses, in ... covering a broad range of epitopes to assist with screening and monitoring CMV progression in future clinical settings. ... These reagents are therefore important for future drug and vaccine development. Immudex has currently developed a CMV Dextramer ...
2007). "Preclinical antitumor activity of a novel folate-targeted dual drug conjugate". Mol. Pharm. 4 (5): 659-67. doi:10.1021/ ... Because novel FR-targeted therapies are now being tested clinically, having the ability to screen patients for FR-positive ... These include an invasive tissue-based immunohistochemical assay, and a non-invasive radiodiagnostic approach. The latter ... Targeted drug therapy is advantageous because it deposits the drug at the specific location where it can be most useful in ...
October 2014). "In situ drug-receptor binding kinetics in single cells: a quantitative label-free study of anti-tumor drug ... Many ligand binding assays require a filtration step to separate bound and unbound ligands before screening. A method called ... 2009). Ligand-binding assays development, validation, and implementation in the drug development arena. Hoboken, N.J.: John ... A ligand binding assay (LBA) is an assay, or an analytic procedure, which relies on the binding of ligand molecules to ...
It was discovered in 1966 by M. E. Wall and M. C. Wani in systematic screening of natural products for anticancer drugs. It was ... M.E. Wall; M.C.Wani; C.E. Cook; K.H.Palmer; A.I.McPhail; G.A.Sim (1966). "Plant antitumor agents. I. The isolation and ... Replacement in any position results in much less potent compound than parent compound in other cytotoxicity assay. The E-ring ... Reduced drug-HSA interactions could result in improved activity. Studies have shown that substitution at position 7, 9, 10 and ...
In vitro assays have shown them both to be selective AR agonists and that they inhibit proliferation of several prostate cancer ... Screening of chemical libraries for AR blockers led to the discovery of the first antiandrogen, cyproterone. An acetate group ... These drugs may therefore be effective as a second-line therapy for refractory prostate cancer previously treated with ... "Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study". Lancet. 375 (9724): 1437-46. doi: ...
... technical barriers to screening natural products in high-throughput assays]. The growing appreciation of functional assays and ... One example of successful use of this strategy is the screening for antitumor agents by the National Cancer Institute, which ... Zheng, Wei; Thorne, Natasha; McKew, John C. (2013). "Phenotypic screens as a renewed approach for drug discovery". Drug ... "The drug development process. Step 4: FDA drug review". US Food and Drug Administration. 4 January 2018. Retrieved 18 December ...
... several assays have been performed to understand the mechanism of Herceptin resistance with/without supplementary drugs. ... November 2017). "Cooperative antitumor activities of carnosic acid and Trastuzumab in ERBB2+ breast cancer cells". J Exp Clin ... As a result, regular cardiac screening with either a MUGA scan or echocardiography is commonly undertaken during the ... "Drug Approval Package: Herzuma". U.S. Food and Drug Administration (FDA). 7 February 2019. Retrieved 28 July 2020. Balduzzi S, ...
Male and female animals underwent a standardized phenotypic screen to determine the effects of deletion. Additional screens ... Yeast three-hybrid assays have shown that this protein binds to the stem loops within the 3'UTR of the POLB mRNA, however the ... and drug resistance. The mitochondrial DNA of mammalian cells is constantly under attack from oxygen radicals released during ... impact on sensitivity towards antitumor agents". Oncogene. 20 (43): 6181-7. doi:10.1038/sj.onc.1204743. PMID 11593426. ...
... rationale and design of screening assays, and the application of such assays for screening of natural product extracts and the ... Antisense drugs are based on the fact that antisense RNA hybridizes with and inactivates mRNA. These drugs are short sequences ... Then, the PD-1 targeted sd-rxRNA helped increasing the anti-tumor activity of tumor-infiltrating lymphocytes (TIL) against ... Sahin U, Karikó K, Türeci Ö (October 2014). "mRNA-based therapeutics--developing a new class of drugs". Nature Reviews. Drug ...
DNA-Interactive Alkylating Agents and Antitumour Platinum-Based Drugs. John Wiley & Sons, Ltd. doi:10.1002/0470025077.chap84b. ... and hence it has been recommended that the babies be screened.[96] ... "ARK™ Methotrexate Assay". Ark Diagnostics.. *^ "Customizing Chemotherapy for Better Cancer Care". My Care Diagnostics.. ... Antibody-drug conjugates[edit]. Antibody-drug conjugates (ADCs) comprise an antibody, drug and a linker between them. The ...
When anticancer drugs such as doxorubicin accumulate in microvesicles, the drug's cellular levels decrease. This can ultimately ... Several tumor markers accessible as proteins in blood or urine have been used to screen and diagnose various types of cancer. ... Circulating microvesicles isolated from cardiac surgery patients were found to be thrombogenic in both in vitro assays and in ... Like other EVs, they been implicated in numerous physiologic processes, including anti-tumor effects, tumor immune suppression ...
... so researchers collect samples from around the world to analyze and evaluate in drug discovery screens or bioassays. This ... June 2020). Assay Guidance Manual. Bethesda: Eli Lilly & Company and the National Center for Advancing Translational Sciences. ... Other natural products derived from marine animals and under investigation as possible therapies include the antitumour agents ... Drug Discovery - Is Mother Nature still the number one source for promising new drugs? Patrick GL (2013). "12.4.2: Medical ...
2008). Analogous successful use of IMC to determine the effects of antitumor drugs on tumor cells in culture within a few hours ... If absolute data are required (e.g. quantity of product produced by a process), then assays can be conducted in parallel on ... This is especially useful for comparative screening-e.g. the effects of different combinations of material composition and/or ... Also, IMC not only documents the general metabolic decline over time due to the drugs, but also the overall frequency of worm ...
Ther Drug Monit. 36 (1): 93-99. doi:10.1097/FTD.0b013e3182a04fc7. PMID 24061446. S2CID 21072472. "ARK Methotrexate Assay". Ark ... DNA-Interactive Alkylating Agents and Antitumour Platinum-Based Drugs". The Cancer Handbook. John Wiley & Sons, Ltd. doi: ... and hence it has been recommended that the babies be screened. Between 30 and 40 percent of people undergoing chemotherapy ... drug-to-drug interactions, genetics, and obesity, which have major impacts on the actual concentration of the drug in the ...
"Abraxane Drug Information Archived 2005-05-26 at the Wayback Machine." Food and Drug Administration. January 7, 2005. Retrieved ... In general, in vitro assays involving microtubules, such as motility assays, rely on paclitaxel to maintain microtubule ... The discovery of paclitaxel began in 1962 as a result of a NCI-funded screening program. A number of years later it was ... Wani MC, Taylor HL, Wall ME, Coggon P, McPhail AT (May 1971). "Plant antitumor agents. VI. The isolation and structure of taxol ...
... and drug screening applications. Using MitoBloCK-6 and/or PluriSIn # 1 the differentiated progenitor cells can be further ... iPSCs have been shown to support the development of all-iPSC mice using a tetraploid (4n) embryo, the most stringent assay for ... They augment anti-tumor responses by producing interferon-gamma (IFN-γ). The approach of collection, reprogramming/ ... of drugs, and toxicity testing of various drugs. The tissue grown from iPSCs, placed in the "chimeric" embryos in the early ...
19 July 2017 Vaccines promoted as key to stamping out drug-resistant microbes "Immunization can stop resistant infections ... Pregnant women are often screened for continued resistance to rubella. The human papillomavirus vaccine is recommended in the U ... van Oirschot JT, Gielkens AL, Moormann RJ, Berns AJ (June 1990). "Marker vaccines, virus protein-specific antibody assays and ... "Prophylactic vaccines are potent activators of monocyte-derived dendritic cells and drive effective anti-tumor responses in ...
... survivin was expressed in all 60 different human tumour lines used in the National Cancer Institute's cancer drug-screening ... In vitro assays and other tests were also performed to validate the idea of the occurrence of an actual immune response to ... "Survivin-derived peptide epitopes and their role for induction of antitumor immunity in hematological malignancies". Leuk. ... A. Cellular T Cell Response The first evidence of survivin-specific CTL recognition and killing was shown in an assay wherein ...
Quintavalle M, Elia L, Price JH, Heynen-Genel S, Courtneidge SA (July 2011). "A cell-based high-content screening assay reveals ... Cdk5 has been proved to be directly linked with drug abuse. We know that drugs act in the reward system, reaching their action ... Cdk5 is involved in tumor proliferation, migration, angiogenesis and also chemotherapy resistance and anti-tumor immunity. It ... Hence, its relation to drug abuse and more specifically to the reward system, which is triggered by the consumption of drugs. ...
... s are complex mixtures of biological compounds, and unlike the case of drugs, there are no true generic vaccines. The ... Pregnant women are often screened for continued resistance to rubella. The human papillomavirus vaccine is recommended in the U ... van Oirschot JT, Gielkens AL, Moormann RJ, Berns AJ (June 1990). "Marker vaccines, virus protein-specific antibody assays and ... "Prophylactic vaccines are potent activators of monocyte-derived dendritic cells and drive effective anti-tumor responses in ...
Some cationic drugs, such as chloroquine and sertraline, are known as lysosomotropic drugs. These drugs are weak bases that ... During a screen seeking to identify microbial secondary metabolites whose activity mimicked that of two cardiac glycosides, ... In a rabbit contractility assay, bafilomycin was used to pre-treat isolated rabbit aorta. The lipophilic agent xylometazoline, ... Bafilomycins exhibit a wide range of biological activity, including anti-tumor, anti-parasitic, immunosuppressant and anti- ...
... the serum free light chain assay, has recently been recommended by the International Myeloma Working Group for the screening, ... There is support for continuous therapies with multiple drug combinations of antimyeloma drugs bortezomib, lenalidomide and ... they have also been observed to have a direct antitumor effect even in people without known skeletal disease.[citation needed] ... "U.S. Food and Drug Administration (FDA). 5 August 2020. Retrieved 6 August 2020.. This article incorporates text from this ...
One screen of single-gene knockouts identified 48 transcription factors (about 20% of all non-essential transcription factors) ... However, 833 of the genes assayed changed behavior between the wild type and mutant cells, indicating that these genes are ... have tried to invent the synthetic Cdk4/6 inhibitor as Cdk4/6 has been characterized to be a therapeutic target for anti-tumor ... are targeted in cancer therapy as the DNA is relatively exposed during cell division and hence susceptible to damage by drugs ...
This assay evaluates the final dilution that may cause a viral infection in 50% of inoculated eggs. This EID50 assay is used to ... This was shown in a mouse model of renal cancer, in which the anti-tumor effect of SeV was suppressed by reducing the number of ... Drug Discovery. 6 (12): 975-90. doi:10.1038/nrd2422. PMC 7097588. PMID 18049472. S2CID 583709. Albini A, Marchisone C, Del ... Sendai Fluorescence Reporter system that allows to screen cells for finding those that are permissive for Sendai virus ...
A number of similar analogues were found and assayed. Structurally similar series of c-Met inhibitors in which a phenolic hinge ... "Orphan Drug Designation". Merck KGaA, Darmstadt, Germany (Press release). 20 November 2019. Retrieved 8 November 2020.. ... "The discovery of benzanilides as c-Met receptor tyrosine kinase inhibitors by a directed screening approach", Bioorganic & ... offered the first proof that relatively selective c-Met inhibitors could be identified and that the inhibition leads to an anti ...
"Daffodil drug's major investment". BBC News. 29 October 2008. Archived from the original on 2008-11-02. Retrieved 2014-10-08. ... These bulbs contain pretazettine, an active antitumor compound. Narcissus products have received a variety of other uses. The ... In Singer (1846) "Wordsworth's Daffodils" (Skip any introductory screen). Wordsworth Trust. Archived from the original on 2014- ... "Detection of Narcissus Latent Virus Isolates Using One-Step Rt-Pcr Assay" (PDF). Journal of Horticultural Research. 21 (1): 11- ...
... antitumor antibiotic - Antiviral drug - anxiolytic - APC - APC vaccine - APC8015 - apheresis - aplastic anemia - aplidine - ... CA 19-9 assay - CA-125 - CA-125 test - cachexia - calcitonin - calcitriol - CAM - Campath-1H - camptothecin - camptothecin ... screening mammogram - Scutellaria barbata - SDX-102 - SDX-105 - second primary cancer - second-line therapy - second-look ... drug tolerance - dry orgasm - DTGM fusion protein - ductal carcinoma - ductal carcinoma in situ - ductal lavage - Dukes' ...
"Drug Screening Assays, Antitumor" by people in this website by year, and whether "Drug Screening Assays, Antitumor" was a major ... Drug Screening Assays, Antitumor*Drug Screening Assays, Antitumor. *Antitumor Drug Screening Assays ... "Drug Screening Assays, Antitumor" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH ( ... Below are the most recent publications written about "Drug Screening Assays, Antitumor" by people in Profiles. ...
The in vitro assays revealed that two naphthalene diimide-polyamine conjugates could inhibit the growth of multiple cancer cell ... Therefore, there is an urgent need for novel drugs with improved efficacy against tumor cells and with less toxicity on normal ... Large-Scale Computational Screening Identifies First in Class Multitarget Inhibitor of EGFR Kinase and BRD4. ... With the aim of up-regulating antitumor efficacy and down-regulating adverse effects, three types of aromatic imide and ...
Different analogues of the antitumor antibiotic rebeccamycin substituted on the imide nitrogen with a methyl group were ... Drug Screening Assays, Antitumor * Enzyme Inhibitors / chemical synthesis * Enzyme Inhibitors / pharmacology * Enzyme ... Their in vitro antitumor activities against murine B16 melanoma and P388 leukemia cells were determined. Their antimicrobial ... Different analogues of the antitumor antibiotic rebeccamycin substituted on the imide nitrogen with a methyl group were ...
Drug Design * Drug Screening Assays, Antitumor * Humans * Lethal Dose 50 * Naphthalenes / chemical synthesis* ... Design and synthesis of C-8 linked pyrrolobenzodiazepine-naphthalimide hybrids as anti-tumour agents Bioorg Med Chem Lett. 2002 ... are prepared with varying degrees of linker length in order to probe the structural requirements for optimal in vitro anti- ...
... factor was used to screen a small molecule library and identify bioactive small molecules with potential antitumor activity. ... A robust p53 cell-based assay that exploits p53s function as a transcription ... Drug Screening Assays, Antitumor. Humans. Mice. Micronuclei, Chromosome-Defective / drug effects. Mitosis / drug effects. ... A robust p53 cell-based assay that exploits p53s function as a transcription factor was used to screen a small molecule ...
1990) New colorimetric cytotoxicity assay for anticancer-drug screening. J Natl Cancer Inst 82: 1107-1112. ... Phenolic; Anti-tumor; Antioxidant; Antimicrobial. Introduction. Main objectives of this study were to evaluate antitumor, ... assay. The results showed that the extract has strong activity against all cell lines tested. The antitumor activity of the ... SRB assay of cytotoxic activity. Human tumor cell lines were obtained frozen in liquid nitrogen (-180°C) from the American Type ...
Drug: paclitaxel Other: antitumor drug screening assay Phase 2 Study Type:. Interventional ... Assay to determine probability of drug resistance to paclitaxel. After successful completion of the EDR assay (approximately 7 ... and low drug resistance to paclitaxel using the Extreme Drug Resistance (EDR) Assay in patients with previously treated ... Assessment of the Predictive Value of the Extreme Drug Resistance (EDR) Assay in Patients Receiving Paclitaxel for Metastatic ...
Drug screening assays antitumor. Necrosis. Propolis. Tumor cells cultured. Resumen en inglés ... Estes resultados sugerem que a atividade antitumor da fração BRVD ocorre com a indução de necrose e os compostos dessa fração ... These results suggest that the antitumor activity of BRVD from red Brazilian propolis occurs through the induction of necrosis ...
DNA Damage / drug effects. Drug Screening Assays, Antitumor. HCT116 Cells. High-Throughput Screening Assays*. Humans. Indoles ... Apoptosis / drug effects*. Cell Line, Tumor. Cell Proliferation / drug effects. Cyclin D / metabolism. Cyclin-Dependent Kinase ... Title: Journal of biomolecular screening Volume: 16 ISSN: 1552-454X ISO Abbreviation: J Biomol Screen Publication Date: 2011 ... Previous Document: Comparison of Multivariate Data Analysis Strategies for High-Content Screening.. Next Document: An Improved ...
Drug Screening Assays, Antitumor. 1. 2011. 792. 0.020. Why? Mitosis. 1. 2013. 1303. 0.020. Why? ...
Drug Screening Assays, Antitumor. MESH. Fibrosarcoma/drug therapy. MESH. Glucans/pharmacology. MESH. ... The in vivo antitumour activity of a beta 1----3/1----6 glucan from the fungus Glomerella cingulata was investigated in vivo. ... The in vivo antitumour activity of a beta 1----3/1----6 glucan from the fungus Glomerella cingulata was investigated in vivo. ... Antitumor and Immunological Activity of a ß-(1.3/1.6) Glucan from Glomerella cingulata ...
Moreover, recent research suggests that EV may represent a natural delivery for molecules including drugs and exosomes may ... represent the ideal natural nanoshuttles for new and old anti-tumor drugs. However, much is yet to be understood about the role ... Moreover, recent research suggests that EV may represent a natural delivery for molecules including drugs and exosomes may ... represent the ideal natural nanoshuttles for new and old anti-tumor drugs. However, much is yet to be understood about the role ...
Drug Screening Assays, Antitumor (130) * Male (129) * Dose-Response Relationship, Drug (100) ... Drugs, July 9, 2010, Vol.70(10), pp.1283-1293 [Peer Reviewed Journal]. ...
Antitumor Drug Screening Assay Undergo pre clinical kinase inhibitor activity screening. Other Name: Drug Screening Assays, ... Antitumor Drug Screening Assay Undergo pre clinical kinase inhibitor activity screening. Other Name: Drug Screening Assays, ... Antitumor Drug Screening Assay Undergo pre clinical kinase inhibitor activity screening. Other Name: Drug Screening Assays, ... Antitumor Drug Screening Assay Undergo pre clinical kinase inhibitor activity screening. Other Name: Drug Screening Assays, ...
Screening for anti-cancer substances iscommonly conducted using viability assays.An inherent problem with this approach isthat ... Tewey KM, Chen GL, Nelson EM, Liu LF: Intercalative antitumor drugs interfere with the breakage-reunion reaction of mammalian ... A Novel High-Through-Put Assay for Screening of Pro-Apoptotic Drugs. ... Screening for anti-cancer substances iscommonly conducted using viability assays.An inherent problem with this approach isthat ...
Drug Screening Assays, Antitumor. MESH. Female. MESH. Humans. MESH. Indoles/chemical synthesis. MESH. ...
Antitumor Angiogenesis Drug Screening in the Zebrafish Model. *Fact or Fiction: Shortcomings and Limitations of the Zebrafish ... As a matter of fact, zebrafish drug screening assays are becoming a reliable tool and are routinely used in preclinical safety ... Antitumor Angiogenesis Drug Screening in the Zebrafish Model. *Fact or Fiction: Shortcomings and Limitations of the Zebrafish ... Antitumor Angiogenesis Drug Screening in the Zebrafish Model. Because of its permeability to small molecules and easy blood ...
... we designed an in vivo drug screening assay in which we tested the effect of anticancer agents on the proportion of MDSC within ... we observed that 5FU had a TLR4-independent antitumor activity (Fig. 3D). These results suggest that the antitumor effects of ... This consideration emphasizes the interest of screening drugs aimed at selectively depleting MDSC. It was recently shown that ... The antitumor effect of 5FU relies on MDSC. A, WT (left) or nude (right) mice were injected with 2 × 105 EL4 cells and treated ...
These cells are used for VIRUS CULTIVATION and antitumor drug screening assays. ...
Drug Screening Assays, Antitumor* (all 22) Animals; Central Nervous System Diseases/drug therapy; Central Nervous System ... Drug Screening Assays, Antitumor*; Eye Diseases/genetics; Female; Genetic Engineering; Heart Diseases/genetics; Heart Diseases/ ... Duchenne/drug therapy; Muscular Dystrophy, Duchenne/genetics; Neoplasms/drug therapy; Neoplasms/genetics; Zebrafish/anatomy & ... Animals; Central Nervous System Diseases/drug therapy; Central Nervous System Diseases/genetics; Disease Models, Animal*; ...
... drug effects; Drug Screening Assays, Antitumor; Enzyme Inhibitors--chemical synthesis; Enzyme Inhibitors--chemistry; Enzyme ... Using a chemical complementation assay, we found that NSC 663284 blocked cellular Erk dephosphorylation caused by ectopic ...
New colorimetric cytotoxicity assay for anticancer-drug screening. J. Natl. Cancer Inst., 82: 1107-1112, 1990. ... Cell Proliferation Assay.. Stock cultures of breast cancer cell lines MCF-7, T-47D, ZR-75-1, BT-474, MDA-MB-231, MDA-MB-453, ... HDAC Assay.. Total cellular extracts were prepared from each breast cancer cell line (14) . All procedures were performed at 4° ... In vitro HDAC activity was assayed as described previously (14 , 15) . Briefly, 20 μl of crude cell extract (∼2.5 × 105 cells ...
Combined drug-screening assays identified teniposide as an ICD drug. ICD drug screening has been reported by several groups, ... The combination of such drugs with immunotherapy, i.e., anti-PD1, may enhance the antitumor efficacy and expand the benefit of ... T cell-based drug screening identified ICD inducers. (A) Outline of drug-screening protocol. B16-OVA tumor cells were seeded on ... we performed drug screenings based on both an ICD reporter assay and a T cell activation assay. We showed that teniposide, a ...
... we performed drug screenings based on both an ICD reporter assay and a T cell activation assay. We showed that teniposide, a ... Furthermore, teniposide potentiated the antitumor efficacy of anti-PD1 in multiple types of mouse tumor models. Our findings ... We also developed a drug-dependent ADP-ribosylation assay in primary cells that correlated with tagraxofusp activity and may ... After screening more than 150 class II-restricted epitopes, we found that myosin heavy chain α (MYHCA) was a dominant cardiac ...
... drug screening assays, antitumor MeSH E05.337.550.200.800 - tumor stem cell assay MeSH E05.337.550.200.900 - xenograft model ... drug screening assays, antitumor MeSH E05.200.500.388.930 - tumor stem cell assay MeSH E05.200.500.410 - electroporation MeSH ... multiphasic screening MeSH E05.318.308.250.580.580 - neonatal screening MeSH E05.318.308.250.580.925 - vision screening MeSH ... antitumor assays MeSH E05.337.550.200.900.830 - subrenal capsule assay MeSH E05.337.550.400 - microbial sensitivity tests MeSH ...
We hypothesize that screening small-molecule libraries highly enriched for FDA-approved drugs will provide a more rapid path to ... We used a homogenous proximity assay to screen for compounds that disrupt the binding of EWS-FLI1 to its cognate DNA targets. A ... which can profoundly alter antitumor drug activity. To address this limitation, we developed the tumor cell-specific in vitro ... Apr, 2010 , Pubmed ID: 20228816 Conventional anticancer drug screening is typically performed in the absence of accessory cells ...
Skehn P et al (1990) New colorimetric cytotoxicity assay for anticancer drug screening. Natl Cancer Inst 82:1107CrossRefGoogle ... Sharma A, Straubinger RM, Ojima I, Bernacki RJ (1995) Antitumor efficacy of taxane liposomes on a human ovarian tumor xenograft ... Vichai V, Kirtikara K (2006) Sulforhodamine B colorimetric assay for cytotoxicity screening. Nat Protoc 1:1112-1116CrossRef ... In vitro drug release study showed initial burst release followed by sustained release for more than 72 h at physiological ...
... drug screening assays, humans, models, neoplasms, antitumor, Pharmacy and materia medica, Drug Discovery, Pharmacology. ... The discovery of anti-cancer drugs has become dependent on cell lines, which are used to screen potential compounds for ... In the future, anti-cancer drug development is likely to use a combination of molecular, cell line, primary or early passage ... and xenografts to improve the accuracy of results during drug development. Over the last few years, there has been an ...
... we used the September 2003 release of the NCI antitumor drug screening database. The data were obtained from the NCI DTP ... inhibition after 48 h of drug treatment had been assessed from changes in total cellular protein using a sulforhodamine B assay ... Some practical consideration and applications of the National Cancer Institute In Vitro Anticancer Drug Discovery Screen. Drug ... Karyotypic complexity of the NCI-60 drug-screening panel. Cancer Res 2003;63:8634-47. ...
ESC-2 had the similar antitumor effect to that of ESC in vivo and further confirmed that ESC-2 may be the main antitumor active ... According to the effect strength, dose and antitumor spectrum, the order of antitumor effects of ESCs was: ESC-2 > ESC > ESC-1 ... 9 enzyme activities were detected by colorimetric assay, Fas, Fas-L, TNF-R1 and TNF-α expression were determined with elisa ... assay and radioimmunoassay respectively. The results showed that ESC, ESC-2 all had inhibitory effects on 4 tumor cells. ...
  • An assay is an investigative (analytic) procedure in laboratory medicine, pharmacology, environmental biology and molecular biology for qualitatively assessing or quantitatively measuring the presence, amount, or functional activity of a target entity (the analyte). (
  • The in vivo antitumour activity of a beta 1----3/1----6 glucan from the fungus Glomerella cingulata was investigated in vivo. (
  • To investigate whether conventional anticancer agents were also able to affect the biology of MDSC, we designed an in vivo drug screening assay in which we tested the effect of anticancer agents on the proportion of MDSC within tumor-bearing mice. (
  • The purpose of this study was to evaluate the antiproliferative and HDAC inhibitory activity of TSA in vitro in human breast cancer cell lines and to assess its antitumor efficacy and toxicity in vivo in a carcinogen-induced rat mammary cancer model. (
  • In randomized controlled efficacy studies using the N- methyl- N- nitrosourea carcinogen-induced rat mammary carcinoma model, TSA had pronounced antitumor activity in vivo when administered to 16 animals at a dose of 500 μg/kg by s.c. injection daily for 4 weeks compared with 14 control animals. (
  • The present studies confirm the potent dose-dependent antitumor activity of TSA against breast cancer in vitro and in vivo , strongly supporting HDAC as a molecular target for anticancer therapy in breast cancer. (
  • ESC-2 had the similar antitumor effect to that of ESC in vivo and further confirmed that ESC-2 may be the main antitumor active fraction of ESC, which was consistent with our previous results in vitro . (
  • Active compounds were tested in mice to determine the maximum tolerated dose, followed by in vivo testing in a hollow fiber assay. (
  • This" multicellular resistance" reflects the relative intrinsic drug-resistant phenotype of most solid tumors growing in vivo and is due to factors such as limited drug penetration or reduced fractions of proliferating cells. (
  • Hence, this compound has the potential to circumvent multicellular drug resistance and, as such, may show promising activity against solid tumors with low growth fractions in vivo , which are frequently intrinsically resistant to conventional cytotoxic anticancer drugs. (
  • The rationale is that if a drug demonstrates antitumor activity in a spheroid model or screen comparable to or greater than that seen in a conventional monolayer system, it could indicate more promising efficacy for the treatment of solid tumors in vivo . (
  • In vivo methods of screening investigative anticancer drugs, biologic response modifiers or radiotherapies. (
  • The development and clinical application of 2-methoxyestradiol (2-ME) as a new type of antitumor drug are limited due to its poor solubility, rapid metabolism in vivo, and large oral dosage. (
  • The present study was carried out to assess the antitumor efficacy of Androctonus australis crude venom using both in vitro and in vivo approaches. (
  • The in vivo assay was carried out by the I.P. transplantation of EAC into Swiss albino female mice, followed by the I.P. injection of the venom at the sublethal dose 1/10 LD 50 (0.025 mg/kg BW) compared to cisplatin (2 mg/kg BW), and both normal and EAC control groups were also included. (
  • The results revealed that the A. australis venom exhibited in vitro and in vivo antitumor activities. (
  • Our goal is to bridge this experimental gap by establishing and characterizing an in vitro/in vivo model useful for examining WDLPS/DDLPS molecular pathogenesis and also therapeutic screening and testing. (
  • In in vivo tumor xenograft mouse models established either by PAT-resistant A549 cells or by patient primary tumors, PAT significantly decreased the tumor volume and tumor weight of NSCLC xenografts at dosage of 40 mg/kg (i.p., daily) and, more importantly, augmented the antitumor efficacy of cisplatin chemotherapy. (
  • A poor correlation between DTD activity and antitumor activity in vitro as well as in vivo was obtained. (
  • Chemosensitivity testing is an ex vivo means of determining or enhancing the cytotoxic and/or cytostatic, or apoptosis-inducing effects of anticancer drugs. (
  • A companion volume, Volume 1: In Vitro Assays contains in vitro and in vivo techniques to identify which new agents or combination of agents are effective for each type of tumor. (
  • Cutting-edge and highly practical, the two volumes of Chemosensitivity provide a comprehensive collection of readily reproducible techniques for the in vitro and in vivo screening of new agents and a set of proven approaches to understand mechanistically why certain cancer cell lines (in vitro) of tumors (in vivo) are more or less sensitive to a particular agent. (
  • Using a high-throughput, unbiased screening approach, we have identified 4′-bromo-3′-nitropropiophenone (NS-123) as a radiosensitizer of human glioma cells in vitro and in vivo . (
  • We have optimized systems of both in vitro and in vivo assays to evaluate the antitumor effects of novel compounds on cell proliferation, apoptosis, differentiation, cellular senescence, colony forming efficiency, and tumorigenicity. (
  • A high-throughput screen with isogenic PTEN+/+ and PTEN-/- cells identifies CID1340132 as a novel compound that induces apoptosis in PTEN and PIK3CA mutant human cancer cells. (
  • Drug induced killing was observed by induction of apoptosis. (
  • Moreover, we use MTT assay which is colorimetric assay, sensitive in vitro for measuring cell proliferation or apoptosis. (
  • en] OBJECTIVE: Chronic lymphocytic leukemia (CLL) cells develop chemoresistance over time associated with defects in apoptosis pathway. (
  • Inhibitors of topoisomerase II are important drugs used in the therapy of many neoplasms including breast cancer, lung cancer, testicular cancer, lymphomas and sarcomas. (
  • Their in vitro antitumor activities against murine B16 melanoma and P388 leukemia cells were determined. (
  • Unexpectedly, the majority of the highest ranking hit compounds from this screen arrest cells in mitosis and most of them impair polymerization of tubulin in cells and in vitro. (
  • This molecule is significantly more potent than the original hit JJ78:1, as it is active in cells at two-digit nanomolar concentrations and shows clear antitumor activity in a mouse xenograft model as a single agent. (
  • RATIONALE: Drugs used in chemotherapy use different ways to stop tumor cells from dividing so they stop growing or die. (
  • Because inactivation of PTEN is a somatic event, PTEN mutations represent an important genetic difference between cancer cells and normal cells and therefore a potential anticancer drug target. (
  • In an effort to identify small molecules that preferentially kill cells with mutations of PTEN, the authors developed and implemented a high-throughput, paired cell-based screen composed of parental HCT116 cells and their PTEN gene-targeted derivatives. (
  • Taken together, these data validate a cell-based screening approach for identifying lead compounds that target cells with specific tumor suppressor gene mutations and describe a novel compound with preferential killing activity toward PTEN and PIK3CA mutant cells. (
  • We show that this assay detectsapoptosis in epithelial cells and that thesensitivity is sufficient for screening inthe 96-well format. (
  • To date, the majority of the antiangiogenesis drug studies have been performed using endothelial cells isolated from either capillaries or large vessels. (
  • These cells are used for VIRUS CULTIVATION and antitumor drug screening assays. (
  • We and others have previously reported that some anticancer agents, in addition to their direct cytotoxic effects on tumor cells, feature the ability to promote the activation of the immune system of the host, resulting in enhanced antitumor responses ( 16 , 17 ). (
  • We also observed that 5FU-mediated MDSC depletion triggered an increase in IFN-γ production by tumor-specific CD8 + T cells infiltrating the tumor bed and promoted a T-dependent antitumor effect. (
  • Brief heating of these drugs-treated cells at 65° for 10 min resulted in a rapid reduction in the number of protein/DNA complexes. (
  • Apoptotic rates of the cancer cells retrieved from the hollow fibers were measured with flow cytometric analysis, caspase 3, 8, 9 enzyme activities were detected by colorimetric assay, Fas, Fas-L, TNF-R1 and TNF-α expression were determined with elisa assay and radioimmunoassay respectively. (
  • The screening of antitumor agents against pancreatic cancer (PC) involves the use of established cell lines, cancer stem cells and spheroids that mimic the patient's tumor. (
  • Almost all known conventional cytotoxic anticancer drugs are less effective in killing tumor cells grown as multicellular spheroids than in killing tumor cells grown as monolayer cell cultures. (
  • Taken together, the results indicate that unlike most other known anticancer cytotoxic drugs, PS-341 appears to be as effective in killing tumor cells grown in the form of multicell spheroids as in killing tumor cells grown in monolayer cell culture. (
  • Depletion of CD8+ T-cells abrogated the antitumor response to the combination therapy. (
  • Tumor acidosis represents an important mechanism mediating drug resistance thus the identification of drugs active on acid-adapted cells may improve the efficacy of cancer therapy. (
  • Here, we characterized human colon carcinoma cells (HCT116) chronically adapted to grow at pH 6.8 and used them to screen the Prestwick drug library for cytotoxic compounds. (
  • The screen led to the identification of several compounds which were further selected for their preferential cytotoxicity towards acid-adapted cells. (
  • Our study provides an example and a tool to identify anticancer drugs targeting acid-adapted cancer cells. (
  • The screening of the Prestwick library compounds led to the identification of the photosensitizer Verteporfin (VP) as an effective compound with preferential activity towards cells in acidic conditions. (
  • Preferential antitumor effect of the Src inhibitor dasatinib associated with a decreased proportion of aldehyde dehydrogenase 1-positive cells in breast cancer cells of the basal B subtype. (
  • Additive antitumor activity of dasatinib and Eto in MDA-MB-231 cells. (
  • Interestingly, the drug was more effective under static conditions compared to when nutrients were flowing through the tumor cells. (
  • Ryuji Yokokawa, who lead the team, explains that the unexpected results prove that we need to consider the balance between proliferation of tumor cells and the efficacy of the drug under flow conditions. (
  • New medications are now tested for safety on specialised cells generated in large numbers from stem cell lines - reducing the need for animal testing - and cancer stem cell lines are used to screen potential anti-tumour drugs. (
  • Thus, there are considerable efforts in adopting stem cell assays for drug discovery, since stem cells can differentiate into specific cell types that may not be available from human sources. (
  • Also, many available human cells have not been very good at predicting side-effects of newly discovered drugs as they enter the pipeline. (
  • In each example, however, it still must be proven that differentiated cells (derived from stem cells) are equivalent to the desired or target cells and can be validated as a drug screening tool. (
  • Patient-specific iPSCs can offer a supply of genetically identical cells that can be differentiated into all somatic cell types for potential use in regenerative therapies or drug screening and testing. (
  • O ne of the key features of current phenotypic approaches is the biological relevance of the assay systems deployed and in this respect the commercial availability of unlimited quantities of pure human cell types, particularly those derived from induced pluripotent stem cells, is having an impact. (
  • Stem cells are fuelling the development of many new disease models and with high levels of translation to human biology and disease these phenotypic assays are increasingly being used in early toxicity testing. (
  • One of the key features of current phenotypic approaches is the biological relevance of the assay systems deployed and in this respect the commercial availability of unlimited quantities of pure human cell types, particularly those derived from induced pluripotent stem cells, is having a major impact. (
  • The assay types that best fit within survey respondents' definition/understanding of phenotypic screening assays were assays involving co-cultures of primary cells and assays involving primary cell cultures (both with 81% selecting). (
  • Apoptotic potential was determined on S-180 cells and drug toxicity was assessed in normal and tumor bearing mice. (
  • First of all, cancer cell line is extracted from the culture media and incubation of these cancer cells with tested drugs or compounds. (
  • The gene expression and the drug resistance property of CD133 positive cancer stem cells, however, are still unknown. (
  • The toxicity of these Pt(II) complexes on noncancer cells was, in all cases, found to be reversed upon drug removal. (
  • We screened a library of clinically relevant compounds at wide dose range and identified Ponatinib and AMG-47a as two candidate compounds that selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells. (
  • Taken together, our results characterized the novel antiangiogenic and antitumor function of PAT in NSCLC cells. (
  • The means by which a drug exerts its effects on cells or tissues. (
  • Neither the presence of a positive IGRA result nor the magnitude of the assayed immune response (IFN-γ (IU·mL −1 ) in the ELISA or number of spot forming cells per 250,000 PBMC in the ELISPOT) was able to discriminate between active TB and LTBI. (
  • Another approach to identify tumor-specific radiosensitizers is to use a cell-based assay, in which the target may not be immediately known but a functional end point (e.g., killing transformed but not normal cells) is used to screen for and identify promising candidates. (
  • The effects of valproic acid (VPA), an antiepileptic drug with histone deacetylase inhibitory activity, on mononuclear cells isolated from 40 CLL patients were evaluated. (
  • However, developing drugs targeting these checkpoint proteins has proved to be quite challenging as cell-based assays used to screen for functional drugs are often difficult to create, involve the use of human primary cells, and have long, complicated protocols. (
  • These mechanism of action-based, biologically relevant, cell-based assays do not require human primary cells and have an easy-to-use protocol, providing a highly sensitive response in less than 5 hours. (
  • Tumor cells deficient in the proapoptotic proteins Bak and Bax are resistant to chemotherapeutic drugs. (
  • These mechanism of action-based, cell-based assays do not require human primary cells, and provide a highly sensitive response, with an easy-to- use protocol that delivers results in a day. (
  • In vitro screen of a small molecule inhibitor drug library identifies multiple compounds that synergize with oncolytic myxoma virus against human brain tumor-initiating cells. (
  • Since traditional subcutaneous xenograft models do not faithfully reproduce the biology of human brain tumors and are often associated with failure or reduced efficacy of the drug/therapy in clinical trials, we are actively engaged in the development of novel orthotopic xenograft models in SCID mice by injecting a patient's tumor cells directly into matched location in mouse brains. (
  • After 30 min, the cells Local assays book washed twice and mixed with 50 ul diluted rabbit anti rat Ig (as facilitating antibody) for 5 min. (
  • A ) From a whole-cell immunodetection assay, we selected 139 cell-permeable compounds that caused increases in phosphonucleolin staining in A549 cells ( 4 ). (
  • Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. (
  • PS-341 has been found to have good broad-spectrum cytotoxic activity in the 60-monolayer cell line National Cancer Institute screen. (
  • The cytotoxic activity of VP was enhanced by light activation and acidic pH culture conditions, likely via increased acid-dependent drug uptake. (
  • To clarify this finding and further investigate combined antitumor effects of dasatinib with cytotoxic agents, a panel of breast cancer cell lines of various subtypes was treated with dasatinib and/or chemotherapeutic agents. (
  • Similarly, cyclophosphamide (CYTOXAN®) is also a cytotoxic drug by cross-linking of strands of DNA and RNA with their alkyl group. (
  • In our paper, we identified the cytotoxic actions of both drugs in vitro by using the chemosensitivity assay. (
  • For in vitro assay, the cytotoxic effect of different venom concentrations was determined against HCT116, HepG2, MCF-7, and PC-3 as cancer cell lines and normal WISH cell line. (
  • Several polynuclear Pt(II) chelates with biogenic polyamines were synthesized and screened for their potential antiproliferative and cytotoxic activity in different human cancer cell lines. (
  • Mitomycin C (MMC) is a clinically used anticancer drug that is reduced to cytotoxic metabolites by cellular reductases via a process known as bioreductive drug activation. (
  • The mode of cytotoxic drug action was determined by annexin binding, DNA fragmentation, and caspase activation. (
  • Screening for anti-cancer substances iscommonly conducted using viability assays.An inherent problem with this approach isthat all compounds that are toxic andgrowth inhibitory, irrespective ofmechanism of action, will score positive.It would be beneficial to be able to screenfor compounds that specifically induceapoptosis. (
  • The discovery of anti-cancer drugs has become dependent on cell lines, which are used to screen potential compounds for activity as well as to explore cancer biology. (
  • Screening data for ∼43,000 nonproprietary compounds are publicly available. (
  • According to this attractive model, we screened microbial cultures, plant extracts, and synthetic compounds for their ability to induce topoisomerase-mediated DNA cleavage in a purified enzyme assay system. (
  • Mixture-based synthetic combinatorial libraries (SCLs) representing hundreds of thousands to millions of individual compounds were screened against the cell-based assay, which evaluates compounds for their ability to inhibit the growth of 60 different human tumor cell lines. (
  • This study demonstrates for the first time the use of in vitro cell-based assays to identify antitumor lead compounds from mixture-based combinatorial libraries. (
  • These implements have advanced the ability to identify target molecules that serve as points of attack for future medicines, the design and synthesis of potential lead compounds, and further characterization, screening, and assays for therapeutic efficacy and toxicity. (
  • In Ligand-Macromolecular Interactions in Drug Discovery: Methods and Protocols, experts in the field highlight the main principles and methodologies currently utilized in the study of molecular interactions between compounds, either natural or synthetic, and complementary biological targets, within the scope of drug discovery. (
  • SPR in Drug Discovery: Searching Bioactive Compounds in Plant Extracts / Anna Rita Bilia -- 14. (
  • Drug screening for the identification of compounds with anticancer activity is commonly performed using cell lines cultured under normal oxygen pressure and physiological pH. (
  • We devised a high-throughput screen for compounds that kill Mtb when its replication has been halted by reactive nitrogen intermediates (RNIs), acid, hypoxia, and a fatty acid carbon source. (
  • Cell-based assays formats play a role in testing compounds for effects on proliferation and screening for inhibitors or modulators of cell growth. (
  • Significant tumor growth retardation by the compounds was noted in early and advanced disease groups, as the life span of drug treated mice increased considerably. (
  • Overall data holds promise for the antitumor activity with lower toxicity of the compounds that can be utilized for the treatment of human malignant tumors. (
  • The compounds showed no cytotoxicity at 10 μM in a zone assay. (
  • This proof-of-principle study demonstrates that it is feasible to use a high-throughput screen to identify compounds that promote the degradation of the Ras oncoprotein as a new approach to target Ras. (
  • RESULTS: A set of 800 small organic compounds was screened for anticancer activity by this cell-based assay, with consumption of each compound at 500 ng. (
  • These results show the potential of this cell-based, high-throughput screening method to identify novel radiosensitizers and suggest that NS-123 and similar nitrophenol compounds may be effective in antiglioma modalities. (
  • This approach has the added benefits of being able to screen a much larger pool of compounds that have been preselected to conform to desirable pharmacologic properties, as well as the opportunity to ultimately identify novel targets for radiosensitization. (
  • Using the U251 human glioma cell line, we initially investigated the radiosensitizing capability of 870 compounds within a commercially available chemical library (Nanosyn, Inc.). We present here the preclinical evaluation of a compound identified in this initial screen, 4′-bromo-3′-nitropropiophenone (NS-123). (
  • To compare the performance of two interferon γ release assays (IGRAs) and conventional screening tests in patients with inflammatory arthritis undergoing screening for latent tuberculosis infection (LTBI) before treatment with anti-tumour necrosis factor α (anti-TNFα) compounds. (
  • We are particularly interested in establishing pre-clinical rational for clinical trials of various antitumor compounds. (
  • Murine Local Lymph Node Assay: A Test Method For Assessing The Allergic Contact Dermatitis Potential Of Chemicals/compounds [Stokes, William S., Hill, Richard N.] on *FREE* shipping on qualifying offers. (
  • Rationale and Strategies for In Vitro Local assays book Assays Early identification of potential genotoxic issues with candidate compounds is an essential part of a product development process. (
  • A combination of two phenotype-based screens, one based on a specific posttranslational modification, the other visualizing microtubules and chromatin, was used to identify compounds that affect mitosis. (
  • To identify cell-permeable small molecules that target other mitotic proteins, we developed the screening strategy in ( Fig. 1 A). First, we used the versatile whole-cell immunodetection (cytoblot) assay ( 2 ) to identify compounds that increase the phosphorylation of nucleolin. (
  • Using this assay, we selected 139 compounds from a library of 16,320 small molecules ( Fig. 1 ) ( 4 ). (
  • Fifty-two compounds inhibited tubulin polymerization ( Fig. 1 B) ( 6 ), and one stimulated tubulin polymerization, like the drug Taxol ( 7 ). (
  • Many natural compounds have led to the discovery of drugs used to treat human disease. (
  • Larsson R, Nygren P: Pharmacological modification of multidrug resistance (MDR) in vitro detected by a novel fluorometric microculture cytotoxicity assay. (
  • SRB cytotoxicity assay in OVCAR-3 cell line revealed Pac-Top free (20:1, w/w) to be more toxic (GI 50 = 6.5 μg/ml) than positive control (Adriamycin, GI 50 = 9.1 μg/ml) and FR-targeted PEGylated liposomes GI 50 (14.7 μg/ml). (
  • Individual cellular "Transpo-mAb" clones isolated by single cell sorting and capable of expressing membrane-bound as well as secreted human IgG were directly screened during antibody discovery, not only for high affinity binding to human ROR2, but also functionally as ADCs using a cytotoxicity assay with a secondary anti-human IgG-toxin-conjugate. (
  • GPC Spin Column HPLC-ESI-MS Methods for Screening Drugs Noncovalently Bound to Proteins / Marsball M. Siegel -- 16. (
  • Inhibition of colony stimulating factor-1 receptor improves antitumor efficacy of BRAF inhibition. (
  • Combined BRAF and CSF-1R inhibition resulted in superior antitumor responses compared with either therapy alone. (
  • Furthermore, in the in vitro angiogenic assays, PAT exhibited dose-dependent inhibition of HUVEC proliferation, migration, and tube formation in response to different stimuli. (
  • Furthermore, the EGFR (epidermal growth factor receptor) and tubulin inhibition assays were carried out for the highest active derivatives to reveal the expected mechanism of action. (
  • In recent years, there has been a growing interest in aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) because of their promising antineoplastic properties. (
  • Thus, this assay would be acceptable as a primary general screen for antineoplastic activity of various crude extracts, as well as for purified fractions, regardless of mode of inhibitory action on tumor formation. (
  • In the future, anti-cancer drug development is likely to use a combination of molecular, cell line, primary or early passage cell culture, and xenograft methods for lead optimisation before clinical trials are contemplated. (
  • Xenograft is once the main the model for anti-tumor drug screening. (
  • Xenograft Model Antitumor Assays" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (
  • This graph shows the total number of publications written about "Xenograft Model Antitumor Assays" by people in this website by year, and whether "Xenograft Model Antitumor Assays" was a major or minor topic of these publications. (
  • Below are the most recent publications written about "Xenograft Model Antitumor Assays" by people in Profiles. (
  • Here, we explore the evidence that has led to the move away from the use of in vitro cell lines and toward various forms of xenograft models for drug screening and development. (
  • I. Prioritize active/aberrant kinase pathways using an in vitro inhibitor screen using individual primary leukemia samples. (
  • We report on the potent activity of TSA as an inhibitor of proliferation and HDAC activity in human breast cancer cell lines and antitumor efficacy without measurable toxicity in the NMU carcinogen-induced rat mammary carcinoma model. (
  • A Scintillation Proximity Assay for Fatty Acid Amide Hydrolase Compatible with Inhibitor Screening / Philip Janes -- 17. (
  • We used the syngeneic mouse model of BRAF (V600E) -driven melanoma SM1, which secretes CSF-1, to evaluate the ability of the CSF-1 receptor (CSF-1R) inhibitor PLX3397 to improve the antitumor efficacy of the oncogenic BRAF inhibitor vemurafenib. (
  • PF-04691502 is an ATP-competitive PI3K/mTOR dual inhibitor, which potently inhibited recombinant class I PI3K and mTOR in biochemical assays and suppressed transformation of avian fibroblasts mediated by wild-type PI3K γ, δ, or mutant PI3Kα. (
  • In summary, PF-04691502 is a potent dual PI3K/mTOR inhibitor with broad antitumor activity. (
  • PF-04691502, a potent ATP competitive PI3K/mTOR dual inhibitor, was discovered through high-throughput screening and structure-based drug design ( 17 ). (
  • To further clarify the combined antitumor effects of dasatinib and Eto, combined treatments with Eto (0.1 μM) with the indicated concentrations of dasatinib were examined in the basal B cell lines. (
  • Some patients may develop a resistance to chemotherapy drugs. (
  • PURPOSE: Phase II trial to determine the reliability of a test for measuring drug resistance to paclitaxel in patients with metastatic breast cancer. (
  • OBJECTIVES: I. Evaluate the proportion of patients with extreme, intermediate, and low drug resistance to paclitaxel using the Extreme Drug Resistance (EDR) Assay in patients with previously treated metastatic breast cancer. (
  • Patients' tumor tissue samples are collected by excisional biopsy, core biopsy, or malignant fluid aspiration, then tested by the Extreme Drug Resistance (EDR) Assay to determine probability of drug resistance to paclitaxel. (
  • Patients whose tumors express resistance to chemotherapeutic drugs tend to do so in one of two ways, either intrinsically or after showing an initial response. (
  • The latter is usually referred to as acquired drug resistance. (
  • Malignant melanoma is an aggressive tumor type that often develops drug resistance to targeted therapeutics. (
  • In an attempt to overcome acidosis-mediated drug resistance, we developed a drug screening assay to target the colon cancer HCT116 cell line chronically adapted to acidosis. (
  • Deregulation of the phosphoinositide 3-kinase (PI3K) signaling pathway such as by PTEN loss or PIK3CA mutation occurs frequently in human cancer and contributes to resistance to antitumor therapies. (
  • These assays enable the development of relevant therapeutics, enabling rapid and sensitive screening of biologics and small molecules. (
  • We used the M30-ELISAassay to screen 500 low molecular weightcompounds from a chemical library from theNational Cancer Institute and identified 16drugs with strong pro-apoptotic activity,suggesting that the assay is a useful toolfor discovery of pro-apoptotic drugs. (
  • Drug discovery remains to be the main focus for biomedical research and represents the essence of antiangiogenesis cancer research. (
  • In vitro cytotoxicity experiment is the first step for screening or discovery of anti-tumor drug. (
  • Ligand-macromolecular interactions in drug discovery : methods and protocols / edited by Ana Cećilia A. Roque. (
  • Beginning with a historical perspective of drug research focusing on the contribution of genomics, proteomics, high-throughput methods, and computational developments in drug discovery, the book then delves into highly detailed methods on topics such as NMR spectroscopy, compound library design and synthesis, chemical and biological microarrays, and many others. (
  • Authoritative and cutting-edge, Ligand-Macromolecular Interactions in Drug Discovery: Methods and Protocols will serve as an ideal guide to scientists in academia and in industry who are striving to further our knowledge of medicines. (
  • An Historical Overview of Drug Discovery / Ana Cecilia A. Roque -- 2. (
  • X-Ray Crystallography in Drug Discovery / Maria Joao Ramos -- 4. (
  • Capillary Electrophoresis in Drug Discovery / Ersilia De Lorenzi -- 13. (
  • A Natural Products Approach to Drug Discovery: Probing Modes of Action of Antitumor Agents by Genome-Scale cDNA Library Screening / Pedro Abreu -- 18. (
  • Improvements in the discovery of natural products along with the emergence of new technologies in cancer screening assays, promise the discovery of new and valuable drugs to tackle pancreatic cancer in the coming years. (
  • Here, we describe the de novo discovery of fully human ROR2-specific antibodies and potent antibody drug conjugates (ADCs) derived thereof by combining antibody discovery from immune libraries of human immunoglobulin transgenic animals using the Transpo-mAb mammalian cell-based IgG display platform with functional screening for internalizing antibodies using a secondary ADC assay. (
  • The screening for functional and internalizing antibodies during the early phase of antibody discovery demonstrates the utility of the mammalian cell-based Transpo-mAb Display platform to select for functional binders and as a powerful tool to improve the efficiency for the development of therapeutically relevant ADCs. (
  • The path to drug discovery is never easy. (
  • While many questions remain, we are happy to have developed this device and have shown that three-dimensional perfused cell culture is vital for the next step in drug discovery . (
  • The promise of stem cell technology as a tool for drug discovery, drug development and as a therapeutic modality is no longer in the future but part of contemporary healthcare. (
  • M ost drug discovery programmes now use functional, cell-based assays for target hit identification and lead optimisation because of the desire to utilise the scientific understanding of signalling pathways. (
  • Pharmaceutical companies have also employed stem cell technology for drug discovery and testing for more than 10 years. (
  • This will hopefully translate into comprehensive drug discovery and development programmes which can bring new medicines to market faster and more cost-effectively. (
  • Phenotypic drug discovery (PDD) implies screening where the molecular mechanism of action is not assumed and does not require knowledge of the molecular target. (
  • As such phenotypic drug discovery is comparable to empirical screening, which was historically used in drug discovery before more target-based approaches became popular. (
  • Currently there is a resurgence in interest in phenotypic drug discovery , driven by many factors, not least the limited success of target-based drug discovery. (
  • P henotypic drug discovery has also been powered by recent advances of high content imaging systems, facilitating the rapid analysis of increasingly complex multi-parametric measurements of cellular phenotypes or biomarkers. (
  • P henotypic drug discovery looks set to be with us for the foreseeable future, with a role alongside targetbased and other approaches to drug discovery. (
  • Phenotypic drug discovery (PDD) was extensively discussed in DDW last year (1) and readers are strongly recommended to consult this excellent review for wider insight. (
  • Repurposing existing drugs not only accelerates drug discovery but rapidly advances clinical therapeutic strategies. (
  • The discovery of new drugs has grown increasingly difficult over the years, as itis a time-consuming, high-investment and high-risk process in traditional drug development. (
  • In the past decade, various high-throughput strategies and experimental platforms have been used for the discovery and identification of repurposable drug candidates, with statins previously identified as potential promising antitumor agents ( 4 ). (
  • Cancer cell lines for drug discovery and development. (
  • This has become such a widespread belief that it approaches dogma in the field of drug discovery and optimization and has spurred a surge in studies devoted to the development of more sophisticated animal models such as orthotopic patient-derived xenografts in an attempt to obtain more accurate estimates of whether particular cancers will respond to given treatments. (
  • Drug research has been greatly transformed by the 'omics revolution' and advances in computational tools, combinatorial chemistry, and high throughput screening techniques (HTS). (
  • A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein. (
  • We generated an EGFP-KRASG12V fluorescence reporter system and implemented it for automated screening in 1536-well plates using high-throughput cellular imaging. (
  • AIM: To develop a leukemia cell line K562-based assay for high-throughput screening. (
  • A cell-based assay was developed to screen for small molecule inducers of intracellular granularity using the HyperCyt high-throughput flow cytometry platform. (
  • Characterization, chemical optimization and anti-tumour activity of a tubulin poison identified by a p53-based phenotypic screen. (
  • A robust p53 cell-based assay that exploits p53's function as a transcription factor was used to screen a small molecule library and identify bioactive small molecules with potential antitumor activity. (
  • It could be demonstrated that a highly ordered structure of the glucan is not essential for the antitumour activity. (
  • In contrast, 19 tumors from 12 TSA-treated rats had a benign phenotype, either fibroadenoma or tubular adenoma, suggesting that the antitumor activity of TSA may be attributable to induction of differentiation. (
  • Dasatinib enhanced antitumor activity of etoposide in the basal B cell lines. (
  • Antitumor activity was observed in U87 (PTEN null), SKOV3 ( PIK3CA mutation), and gefitinib- and erlotinib-resistant non-small cell lung carcinoma xenografts. (
  • Objective: Describe the synthesis and characterization of new vanadium complexes with orotic and glutamic acids, and test its antitumor activity against HepG2 and Caco-2. (
  • Some fluoroquinazolinones ( A - H ) were designed, synthesized and biologically evaluated for their antitumor activity against the two cell lines, MCF-7 and MDA-MBA-231. (
  • New derivative G (IC 50 = 0.44 ± 0.01 µM) showed antitumor activity, better than that of the reference drug erlotinib (IC 50 = 1.14 ± 0.04 µM) against MCF-7. (
  • New derivative E (IC 50 = 0.43 ± 0.02 µM) showed higher activity than the reference drug erlotinib (IC 50 = 2.55 ± 0.19 µM) against MDA-MBA-231. (
  • Drug Screening Assays, Antitumor" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (
  • Elimination of MDSC in mouse tumor models was shown to enhance antitumor responses, resulting in tumor regression. (
  • The in vitro assays revealed that two naphthalene diimide-polyamine conjugates could inhibit the growth of multiple cancer cell lines more potently than amonafide. (
  • In summary, these results identify JJ78:12 as a potential cancer therapeutic, demonstrate that screening for activators of p53 in a cell-based assay is an effective way to identify inhibitors of mitosis progression and highlights p53's sensitivity to alterations during mitosis. (
  • Testing patients' blood or bone marrow to find out if their type of cancer may be sensitive to a specific drug may help doctors choose more effective treatments. (
  • To design new therapeutic strategies and to test the efficacy of antiangiogenic cancer drugs, researchers and clinicians need models in which these malignant angiogenic events can be replicated and then studied at genetic, biochemical, molecular, and cellular levels. (
  • Danhier F, Feron O, Preat V (2010) To exploit the tumor microenvironment: passive and active tumor targeting of nanocarriers for anti-cancer drug delivery. (
  • Advances in the understanding of cancer cell biology and response to drug treatment have benefited from new molecular technologies and methods for integrating information from multiple sources. (
  • Nanodelivery of antitumor drugs is a new treatment mode for cancer. (
  • The device allows researchers to mimic the environment inside the body to screen for better cancer screening drugs. (
  • Kyoto University researchers have developed a new 'tumor-on-a-chip' device that can better mimic the environment inside the body, paving the way for improved screening of potential cancer fighting drugs. (
  • Yuji Nashimoto et al, Vascularized cancer on a chip: The effect of perfusion on growth and drug delivery of tumor spheroid, Biomaterials (2019). (
  • Comparison with established anti-cancer drugs suggested that potential of Nap-NU, Napro-NU and 5-NO 2 -Nap-NU as an anti-cancer agent may be critically examined for their entry in clinical settings. (
  • In this assay, we used MCF-7 breast cancer cell line. (
  • In daily practice, these two drugs are widely used in many cancer therapies. (
  • Chemosensitivity assay may help in choosing the best drug or compound for the cancer being treated. (
  • The anticancer potential of these complexes was studied preliminarily by using MTT assay in cancer and normal cell lines along with the benchmark drugs (cisplatin, carboplatin, and gemcitabine). (
  • However, the antitumor effects of statins on pancreatic cancer and their differential efficacy among a variety of statins are not currently well‑defined. (
  • Moreover, EVs are emerging as natural delivery systems and in particular, exosomes may represent the ideal natural nanoshuttles for new and old anti-tumor drugs. (
  • A drug assay was then performed with the team administrating an anti-tumor drug at low doses. (
  • We hypothesize that at low doses the benefit of the nutrient flow outweighs the effect of the anti-tumor drug. (
  • All drugs were administrated by i.p. injection, except for doxorubicin, which was injected i.v. (
  • 15 16 17 18 19 The limited specificity of TST may result in unnecessary anti-tuberculosis treatment and the risk of significant drug toxicity. (
  • In this study, we developed a cell-based, high-content screening platform to identify small molecules that could promote the degradation of the KRAS oncoprotein. (
  • A further screen of approximately 25,000 small molecules led to the identification of a class of aryl-oxazoles that increased intracellular granularity in both cell lines, often leading to cell death. (
  • However, the validation and selection of primary screening assays, both phenotypic and target-based, are vital to guaranteeing a selection of extracts or molecules with relevant pharmacological action. (
  • Phenotypic assays aim to quantity a phenotype or pathway in a physiological relevant system (typically a cell or whole organism) and make limited assumptions as to the molecular basis of how the system works. (
  • Phenotypic screening includes any screening where the molecular mechanism of action is not assumed and does not involve screening against an isolated target. (
  • Phenotypic assays share a common feature, ie there must be high confidence in their translation to human biology and disease. (
  • This survey set out understand and record the latest thinking around many aspects of PDD, including how it is being deployed, where phenotypic assays are most suited to be used, expectations of phenotypic screening, milestones achieved, future requirements for phenotypic primary screening and assay technologies and instrument platforms currently used in PDD. (
  • The results of the survey were publ ished in HTStec's PPD Trends 2015 report (2) and selected findings are now reported in this article together with vendor updates on technologies facilitating phenotypic screening assays. (
  • Cytoskeleton, Inc. has been a reliable source of compound screening data, custom protein production, assay design & development and antibody/ELISA development for past two decades. (
  • The test, manufactured by Ortho-Clinical Diagnostics (Raritan, New Jersey), is an enzyme-linked immunosorbent assay (ELISA) that uses epimastigote lysate antigens for detection of antibodies to T. cruzi in serum and plasma ( 8 ). (
  • Proteasome inhibitors such as PS-341, a dipeptide boronic acid analogue, represent an interesting new class of potential anticancer drugs, which are entering early-phase clinical trials. (
  • Mechanism-based assays detect potential anticancer agents that interfere with neoplastic growth, or focus on target receptors that were discovered as the mechanism of drug action (McLaughlin, 1991). (
  • These drugs, referred to as topoisomerase poisons, include synthetic intercalators (e.g., mAMSA, mitoxantrone), antibiotics from microbes (e.g., anthracyclines, actinomycin D), and derivatives of plant metabolites [e.g., camptothecin derivatives such as CPT-11 and topotecan and epipodophyllotoxin derivatives such as VP-16 (etoposide) and VM-26 (teniposide)] ( 4-10 ). (
  • Enhanced antitumor efficacy of low-dose Etoposide with oncolytic herpes simplex virus in human glioblastoma stem cell xenografts. (
  • article{Cheema2011EnhancedAE, title={Enhanced antitumor efficacy of low-dose Etoposide with oncolytic herpes simplex virus in human glioblastoma stem cell xenografts. (
  • Nowadays, there are many different types of chemo sensitivity assays to access the sensitivity have been developed. (
  • 12 Conventional screening modalities, including the tuberculin skin test (TST), lack sensitivity and specificity. (
  • As a model drug, pingyangmycin has antitumor and antiangiogenic effects. (
  • It is chemically similar to bleomycin with antitumor and antiangiogenic effects. (
  • Furthermore, the robustness and reproducibility of these assays lend themselves well to use in lead optimization, relative potency, and QC lot release testing of immunotherapy drugs. (
  • Furthermore, the robustness and reproducibility of these assays lend themselves well for use in characterization, relative potency, and QC lot release testing of immunotherapy drugs. (
  • Dose-response curves generated by the screening process provide 50% growth inhibitory (GI 50 ) values for each compound-cell line pair. (
  • The combination index of IC50 was 0.3 or 0.4 in the MDA-MB-231 or MDA-MB-157 cell line, respectively, that is, Eto additively enhanced the antitumor effect of dasatinib in these cell lines (Figures 6 and 7). (
  • There is good evidence that topoisomerases are the principal intracellular targets for a number of clinically important antitumor drugs ( 2 , 3 ). (
  • Here, we present data for assays targeting a number of clinically important immunotherapy targets, including PD-1 (with PD-L1 and PD-L2), ICOS, CD28, BTLA, and OX40. (
  • Here, we present its biochemical and cellular profiles, antitumor efficacy, and pharmacokinetic/pharmacodynamic correlations. (
  • The analysis of ascetic fluid tumor, survival study, and hematological, biochemical, antioxidant, and histopathological assays was evaluated in control and treated animal groups. (
  • The identification of key enzymes responsible for drug activation has been investigated extensively with the ultimate aim of tailoring drug administration to patients whose tumors possess the biochemical machinery required for drug activation. (
  • The analyte can be a drug, biochemical substance, or cell in an organism or organic sample. (
  • In the lymphocyte transformation assay the glucan at a dose of 100 micrograms/ml caused a fourfold increase in the proliferation of murine spleen lymphocytes. (
  • Murine Local Lymph Node Assay: A Test Method For Assessing The Allergic Contact Dermatitis Potential Of Chemicals/compoundsFormat: Paperback. (
  • Screen anticancer drug in vitro using resonance light scattering technique. (
  • Twentyman PR, Luscombe M: A study of some variables in a tetrazolium dye (MTT) based assay for cell growth and chemosensitivity. (
  • Biocompatibility of these polymers was confirmed by methyl tetrazolium assays and scanning electron microscopy. (