• Combination chemotherapy regimens, such as FOLFIRINOX and nab-paclitaxel plus gemcitabine, have demonstrated improved survival rates in advanced pancreatic cancer ( 7 , 8 ). (frontiersin.org)
  • Gemcitabine (dFdC) is an active antitumour agent with radiosensitising properties, shown both in preclinical and clinical studies. (biomedcentral.com)
  • A high-throughput screen indicates gemcitabine and JAK inhibitors may be useful for treating pediatric AML. (createuky.net)
  • With regard to chemotherapy, for approximately 80% of patients with locally advanced or metastatic illness, gemcitabine or 5-fluorouracil chemotherapy provides a survival time of months, and nab-paclitaxel combined with gemcitabine or FOLFIRINOX provides slight improvements [ 10 , 11 ]. (hindawi.com)
  • Tubulin polymerization must also be responsive to polymerization enhancers (paclitaxel) and inhibitors (nocodazole) at 5 µM drug concentration. (cytoskeleton.com)
  • Some Mek inhibitors showed promising antitumor activity, although schedules and doses associated with low systemic toxicity need to be defined. (biomedcentral.com)
  • Finally, several clinical trials are currently ongoing using MEK inhibitors in combination with chemotherapeutic drugs (including dacarbazine or paclitaxel). (biomedcentral.com)
  • Bromodomain-Selective BET Inhibitors Are Potent Antitumor Agents against MYC-Driven Pediatric Cancer. (createuky.net)
  • Molecular defects are often represented by hereditary BRCA (Breast cancer gene) mutations leading to altered DNA repair, thus presuming higher efficiency of DNA-damaging agents, such as platinum drugs and poly-ADP-ribose polymerase (PARP) inhibitors. (cttjournal.com)
  • At present, postoperative platinum drugs and paclitaxel-based chemotherapy is the treatment of gold standard for ovarian cancer. (gentaur-online.com)
  • By addressing the limitations of conventional chemotherapy, such as poor biodistribution, cancer cell drug resistance, and significant systemic adverse effects, NPs hold great promise of drastically transforming the face of oncology[1-2]. (pdfplayer.org)
  • These nanocapsules are made of a PLGA-polymer matrix coated with Fe/FeO core-shell nanocrystals and co-loaded with chemotherapy drug and photothermal agent. (nature.com)
  • Metformin enhances the sensitivity of drug-resistant ovarian cancer cells to chemotherapy. (oncotarget.com)
  • Chemotherapy with platinum drugs such as cisplatin, carboplatin, oxaliplatin, or a combination thereof is used to treat a variety of tumors. (eurekaselect.com)
  • However, the results of gliomas chemotherapy are unsatisfactory, and resistance to platinum drugs is one of the important reasons. (eurekaselect.com)
  • Interferon and the chemotherapy agents dacarbazine, cisplatin, and vinblastine are approved by the US Food and Drug Administration (FDA) for use as adjuvant therapy in melanoma. (medscape.com)
  • Based on this method, we performed cytotoxicity assays on 42 AsPCs grown both as monolayers and spheroids. (biomedcentral.com)
  • The ability of lovastatin, mevastatin and simvastatin to inhibit the melanoma cell proliferation was examined using cytotoxicity and apoptosis assays. (biomedcentral.com)
  • We confirm that in vitro cytotoxicity test MTT assay is able to predict in vivo toxicity, at least for aflatoxins using the prediction model. (lookformedical.com)
  • Scientific Methods: In vitro growth inhibition assays were completed with AHCC alone and in combination with PLD in panel of human cancer cell lines and findings confirmed in vivo in an ovarian cancer xenograft mouse model. (researchgate.net)
  • Major Findings: The in vitro growth inhibition assays demonstrated additive activity when AHCC is co-administered with PLD. (researchgate.net)
  • Integration of a machine learning-derived signature of response with in vitro assessment of LP-184 efficacy facilitated the derivation of manageable yet robust biomarkers which can be used to predict drug sensitivity with high accuracy and clinical value. (biomedcentral.com)
  • We examined the effects of statin drugs on in vitro proliferation, migration and invasion of melanoma cells. (biomedcentral.com)
  • their structures were elucidated using spectroscopic methods and their bioactivity was evaluated using an in vitro microtubule assembly assay. (liverpool.ac.uk)
  • Nanoparticles (NPs) are tailored drug delivery vectors that can selectively target huge dosages of chemotherapeutic drugs or therapeutic genes into cancer cells while leaving healthy cells alone. (pdfplayer.org)
  • Global gene expression comparison of 6 PARPi-resistant and 6 PARPi-sensitive 3D AsPCs was indicative for the predominant downregulation of numerous genes and networks with previously demonstrated roles in EOC chemoresistance, suggesting that the PARPis-sensitive AsPCs could display enhanced sensitivity to other chemotherapeutic drugs, commonly applied in cancer management. (biomedcentral.com)
  • Chemotherapeutic drugs target cancer-specific characteristics, such as alterations in DNA repair, which has complicated roles in oncogenesis and tumor progression. (biomedcentral.com)
  • Platinum drugs are a class of chemotherapeutic drugs that affect the cell cycle, and the main site of action is the DNA of cells, which are common chemotherapeutic drugs in clinical practice. (eurekaselect.com)
  • The diphosphate (dFdCDP) and triphosphate (dFdCTP) forms of the drug play an important role in the cytotoxic effect: dFdCDP is an inhibitor of ribonucleotide reductase, while dFdCTP is incorporated into DNA, both leading to the inhibition of DNA synthesis. (biomedcentral.com)
  • The cell inhibition rate was used to evaluate the inhibitory effect of drugs on the tumor and the effect of adaptation for drug resistance. (oncotarget.com)
  • This study investigated whether BRD4 inhibition can alter the immunomodulatory and antitumor effects of radiation therapy (RT). (preprints.org)
  • Therefore, addition of BRD4 inhibition significantly enhanced the systemic antitumor responses of local RT. (preprints.org)
  • Hits from these screens are then tested in cells and then in animals for efficacy. (wikipedia.org)
  • Modern drug discovery involves the identification of screening hits, medicinal chemistry and optimization of those hits to increase the affinity, selectivity (to reduce the potential of side effects), efficacy/potency, metabolic stability (to increase the half-life), and oral bioavailability. (wikipedia.org)
  • Moreover, after antitumor treatment, [ 89 Zr]Zr-DFO-KN035 enabled observational imaging for therapeutic efficacy evaluation, which can help predict patient prognosis. (thno.org)
  • Finally, the efficacy of certain potential drugs was predicted using the pRRophetic algorithm, and the results in the high- and low-risk groups were compared. (hindawi.com)
  • Efficacy and safety of first-line single-agent carboplatin vs carboplatin plus paclitaxel for vulnerable older adult women with ovarian Cancer: A GINECO/GCIG randomized clinical trial. (eurekaselect.com)
  • drug resistance, and significant systemic adverse effects. (pdfplayer.org)
  • After sequencing of the human genome allowed rapid cloning and synthesis of large quantities of purified proteins, it has become common practice to use high throughput screening of large compounds libraries against isolated biological targets which are hypothesized to be disease-modifying in a process known as reverse pharmacology. (wikipedia.org)
  • The idea that the effect of a drug in the human body is mediated by specific interactions of the drug molecule with biological macromolecules, (proteins or nucleic acids in most cases) led scientists to the conclusion that individual chemicals are required for the biological activity of the drug. (wikipedia.org)
  • This library represents a selection of drug-like compounds aimed at modulating protein-protein interaction (PPI) of β-catenin with different proteins involved in significant physiological processes. (chemdiv.com)
  • Our study shows that the combination of paclitaxel and metformin has synergistic effect on cell survival and suppresses the expression of proteins involved in cancer metastasis. (ksdb.org)
  • In contrast to results with 2D culture, observed mitotic arrest was relatively low, suggesting involvement of additional mechanisms in their antitumor effect in vivo . (nature.com)
  • This mini-review summarizes the resistance mechanisms of gliomas to platinum drugs, as well as molecules and therapies that can improve the sensitivity of gliomas to platinum drugs. (eurekaselect.com)
  • TL238) for anti-tubulin ligand drug discovery. (cytoskeleton.com)
  • In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which new candidate medications are discovered. (wikipedia.org)
  • Historically, drugs were discovered by identifying the active ingredient from traditional remedies or by serendipitous discovery, as with penicillin. (wikipedia.org)
  • Modern drug discovery is thus usually a capital-intensive process that involves large investments by pharmaceutical industry corporations as well as national governments (who provide grants and loan guarantees). (wikipedia.org)
  • Despite advances in technology and understanding of biological systems, drug discovery is still a lengthy, "expensive, difficult, and inefficient process" with low rate of new therapeutic discovery. (wikipedia.org)
  • This approach is known as classical pharmacology, forward pharmacology, or phenotypic drug discovery. (wikipedia.org)
  • EFMC would like to remind his efforts, joint with Henk Timmerman and Han van de Waterbeemd, to launch the successful series of EFMC Short Course in Medicinal Chemistry in 2009 with a very successful course on "Improving Compound Quality: Physical Chemistry and DMPK Properties in Drug Discovery. (efmc.info)
  • Cancer research has been conducted using cultured cells as part of drug discovery testing, but conventional two-dimensional culture methods are unable to reflect the complex tumor microenvironment. (medsci.org)
  • Natural products, which can be isolated from living organisms around the world, have played an important role in drug discovery since ancient times. (gentaur-online.com)
  • On any given day, the media streams are filled with companies announcing their latest biologic achievements in medicine, and given the high profile of these therapeutics in disease areas such as oncology and autoimmunity, it is hardly surprising if some people have forgotten the role of medicinal chemistry in the drug discovery process. (drugdiscoverynews.com)
  • Part of the reason for medicinal chemistry's disappearing act may be due to attempts by the pharmaceutical industry itself to move medicinal chemists to the back burner by automating molecular discovery and synthesis through methods such as combinatorial chemistry and high-throughput screening (HTS). (drugdiscoverynews.com)
  • When I was at GSK and also when I was with Shire , one of the things I really had antibodies to was this whole notion of industrializing drug discovery-at the end of the day, that's really what combinatorial chemistry and HTS is or was-because I really believe that drug discovery of new medicines is truly a creative process," he says. (drugdiscoverynews.com)
  • Discovery pipelines have been horribly inefficient, and if you look at the major pharmas, what they're doing typically is dismantling that industrial framework and moving much more toward either internal-focused discovery with very small discovery units-and that's certainly how GSK's done it-or partnering with academic units or highly creative companies like Ambrx to bring forward those creative molecules as rational drug design from different disciplines converges," he adds. (drugdiscoverynews.com)
  • The discovery of novel antimicrobial drugs is sparked by the emergence of various antibiotic resistance strains. (biomedcentral.com)
  • Targeted cancer therapies are used to inhibit the growth, progression, and metastasis of the tumor by interfering with specific molecular targets and are currently the focus of anticancer drug development. (spandidos-publications.com)
  • Pingyangmycin is an anticancer drug known as bleomycin A5 (A5), discovered in the Pingyang County of Zhejiang Province of China. (lookformedical.com)
  • In its Phase II trial targeting advanced or metastatic bladder cancer, Roche said its atezolizumab immunotherapy drug shrank tumors in 27 percent of people who expressed medium and high levels of PD-L1, a protein that appears to help cancers evade the immune system. (e-cancer.fr)
  • 89 Zr]Zr-DFO-KN035 monitored and predicted the site of adverse reactions in antitumor immunotherapy. (thno.org)
  • As a novel antitumor therapy, tumor immunotherapy is attracting considerable attention and extensive research worldwide. (thno.org)
  • Under the tumor immunotherapy strategy, various monoclonal antibody drugs are being developed and marketed to eliminate tumor cells by suppressing tumor immune-checkpoint signaling pathways and reactivating antitumor immune responses. (thno.org)
  • This review summarizes the intracellular functions of Akt as a pivotal point of converging signaling pathways involved in cell growth, proliferation, apoptotis and neo‑angiogenesis, and focuses on the drug design strategies to develop potent anticancer agents targeting Akt. (spandidos-publications.com)
  • Decreased intracellular drug concentration, enhanced function of cell processing active products, enhanced repair ability of cellular DNA damage, and blockage of related apoptosis pathways play an important role in it. (eurekaselect.com)
  • Cisplatin showed concentration-dependent antitumor effects due to loss of cell adhesion and spheroid disruption in each cell line, while cetuximab exhibited antitumor effects that correlated with EGFR expression in each cell line. (medsci.org)
  • 2013. Brine shrimp lethality assay 'an effective prescreen': Microwave-assisted synthesis, BSL toxicity and 3DQSAR studies-based designing, docking and antitumor evaluation of potent chalcones. (cytoskeleton.com)
  • Thus, the plant may act as a potent antimicrobial drug against resistant strains. (biomedcentral.com)
  • Analysis of mitosis and antimitotic drug responses in tumors by in vivo microscopy and single-cell pharmacodynamics. (nature.com)
  • Additional screens for MMTV provirus entry sites in tumors revealed several other upregulated genes that are associated with other gene development pathways such as INT2, INT3, and INT4 [4,5,6]. (chemdiv.com)
  • Smartly engineered nanocapsules can not only shrink and decompose into small-sized nanodrugs upon drug release but also can regulate the TME to overproduce reactive oxygen species for enhanced synergistic therapy in tumors. (nature.com)
  • Special advances are achieved in HER-positive tumors using targeted therapy with drugs which suppress the tumor cell growth factors (trastuzumab, herceptin). (cttjournal.com)
  • We applied our workflow to quantify cell-cycle effects of three antimitotic cancer drugs over 8 d in HT-1080 fibrosarcoma xenografts in living mice using a data set of 38,000 cells and compared the induced phenotypes. (nature.com)
  • Besides, recent efforts have focused on developing targeted therapies for pancreatic cancer, including drugs that target specific molecular alterations like the KRAS oncogene, which is frequently mutated in pancreatic cancer ( 9 - 11 ). (frontiersin.org)
  • Regardless of the therapeutic approach, the heterogeneity of pancreatic cancer cells and the complexity of its tumor microenvironment contribute to the emergence of drug resistance. (frontiersin.org)
  • Their current application in oncology has revolutionized cancer treatment by improving the antitumor activity of several chemotherapeutic agents. (mdpi.com)
  • In the future, it may become possible to produce tumor spheroids from tissue samples of oral cancer patients, and then apply them to drug screening and to develop individualized diagnostic and treatment methods. (medsci.org)
  • Therapies tailored to specific genetic lesions and diagnostic tests that assay for their respective molecular targets are now an established part of clinical practice across various tumour types, including chronic myeloid leukaemia 1 , gastrointestinal stromal tumours and epithelial tumours, such as breast and colon cancer 2 . (ersjournals.com)
  • Smart drug delivery systems (SDDSs) for cancer treatment are of considerable interest in the field of theranostics. (nature.com)
  • Investors will be probing kidney cancer doctors at this weekend's meeting to see which drug they prefer. (e-cancer.fr)
  • Antibacterial activity was evaluated by using disc and agar diffusion methods and the anti-cancer effect of the rose flower extract (RE) was examined using MTT assay in lung cancer cell line. (biomedcentral.com)
  • Jacob et al [ 9 ] examined the association between use of cholesterol-lowering drugs and colorectal cancer incidence among 132,136 men and women in the Cancer Prevention Study II Nutrition Cohort. (biomedcentral.com)
  • Current or 5 year use of cholesterol-lowering drugs was not associated with colorectal cancer incidence. (biomedcentral.com)
  • Mitsiades CS, Mitsiades N and Koutsilieris M: The Akt pathway: Molecular targets for anti-cancer drug development. (spandidos-publications.com)
  • Curr Cancer Drug Targets. (spandidos-publications.com)
  • This study aims to investigate the association of p53 and D-loop gene with drug resistance and sensitization induced by metformin in ovarian cancer. (oncotarget.com)
  • Then, the inhibitory rate on cells in the experimental group was observed by CCK8 assay, in order to study the sensitization effect of metformin in different chemotherapies of ovarian cancer. (oncotarget.com)
  • From the paper: 'Carriers of pathogenic germline variants (PGV) in BRCA2 could soon be offered gastric cancer screening using gastroscopy. (cdc.gov)
  • In the longer term, some might even take part in lung cancer screening programs. (cdc.gov)
  • Library has been assembled using in house structural biology insight, molecular stimulation-modeling, virtual screening of ChemDiv's novel chemistries and medicinal chemistry filtering/ranking of the resulting hits. (chemdiv.com)
  • The application of this assay and the potential biomarkers with possible predictive significance to PARPis therapy of EOC patients now need testing in the setting of a clinical trial. (biomedcentral.com)
  • The data on the prognostic and predictive role of the tumor molecular biomarkers, as well as on clinically used and cellular therapy approaches and developing targeted drugs are presented, and the prospects for the future research are outlined. (cttjournal.com)
  • Phenotypic Screens Reveal Posaconazole as a Rapidly Acting Amebicidal Combination Partner for Treatment of Primary Amoebic Meningoencephalitis. (createuky.net)
  • Some studies have confirmed that [ 9 - 12 ] metformin could increase chemosensitivity, especially in combination with paclitaxel. (oncotarget.com)
  • These findings suggest that the combination of paclitaxel and metformin can be a possible therapeutic option for treatment of melanoma. (ksdb.org)
  • The resistance of gliomas to platinum drugs is the result of a combination of influencing factors. (eurekaselect.com)
  • miRNAs and lncRNAs control drug sensitivity and the development of tumor resistance towards platinum drugs. (eurekaselect.com)
  • Herbal plants are a promising source of drug targets for various acute and chronic diseases. (biomedcentral.com)
  • Figure 4: Quantitative analysis of drug response to paclitaxel treatment at a single-cell level. (nature.com)
  • Small-molecule osteogenesis-promoting drugs are required to improve the treatment for this disease. (bvsalud.org)
  • Drugs by Bristol-Myers Squibb and Exelixis proved superior in tests to current standard treatment. (e-cancer.fr)
  • The statins are group of drugs routinely used in the treatment of lipid disorders, including hypercholesterolemia. (biomedcentral.com)
  • Arencibia JM, Pastor-Flores D, Bauer AF, Schulze JO and Biondi RM: AGC protein kinases: From structural mechanism of regulation to allosteric drug development for the treatment of human diseases. (spandidos-publications.com)
  • Paclitaxel is currently prescribed for treatment of melanoma. (ksdb.org)
  • Therefore, we reasoned that combined treatment of paclitaxel with metformin could be more effective in the suppression of cell proliferation than treatment of paclitaxel alone. (ksdb.org)
  • It also proved to be well-tolerable drug with low cost for the treatment of diabetic patients. (ksdb.org)
  • Open data on the gene expression of the NCI-60 cell lines, provides a unique opportunity to add another dimension to the preclinical development of such drugs by interrogating correlations with gene expression patterns. (biomedcentral.com)
  • However, developing SDDSs with early diagnostic capability, enhanced drug delivery and efficient biodegradability still remains a scientific challenge. (nature.com)
  • The biological activity of HTS02 is assessed by a tubulin polymerization assay. (cytoskeleton.com)
  • Historically, substances, whether crude extracts or purified chemicals, were screened for biological activity without knowledge of the biological target. (wikipedia.org)
  • His achievements in understanding the role of physiochemical properties in drug activity, more precisely in the disposition of medicines ought to be particularly recognised. (efmc.info)
  • dCK activity of the cells was determined by an enzyme activity assay. (biomedcentral.com)
  • Screening of herbal plants for various therapeutic properties is the hour as it shows promising activity. (biomedcentral.com)
  • Examples of drug compounds isolated from crude preparations are morphine, the active agent in opium, and digoxin, a heart stimulant originating from Digitalis lanata. (wikipedia.org)
  • Later, small molecules were synthesized to specifically target a known physiological/pathological pathway, avoiding the mass screening of banks of stored compounds. (wikipedia.org)
  • With an eye to filling those drying pipelines with an endless supply of potentially therapeutic compounds, companies heavily invested in ways to randomly generate tens of thousands of "drug-like" compounds from the chemical building blocks of known drugs (see sidebar, "Leaving Lipinski? (drugdiscoverynews.com)
  • As the American Chemical Society 's Mark Lesney glibly wrote back in 2002: "A large enough library with the right high-throughput screening assay promised the ultimate brute-force method for obtaining bioactive compounds without biologists and organic chemists getting in the way. (drugdiscoverynews.com)
  • We have developed a 3D (spheroid) functional assay to assess the sensitivity of two PARPis (niraparib and olaparib) in ascites-derived primary cell cultures (AsPCs) from HGSOC patients. (biomedcentral.com)
  • More recently, chemical libraries of synthetic small molecules, natural products or extracts were screened in intact cells or whole organisms to identify substances that had a desirable therapeutic effect in a process known as classical pharmacology. (wikipedia.org)
  • Meanwhile, for disorders whose rarity means that no large commercial success or public health effect can be expected, the orphan drug funding process ensures that people who experience those disorders can have some hope of pharmacotherapeutic advances. (wikipedia.org)
  • Figure 6: Antimitotic drugs induce different mitotic and interphase phenotypes. (nature.com)
  • Single-cell and subcellular pharmacokinetic imaging allows insight into drug action in vivo . (nature.com)
  • From accessing medicines to intellectual property to drug safety, PhRMA is devoted to advancing public policies that support innovative medical research, improve treatments and yield real results. (wgc2010.sk)
  • To be allowed to come to market, drugs must undergo several successful phases of clinical trials, and pass through a new drug approval process, called the New Drug Application in the United States. (wikipedia.org)
  • Once a compound that fulfills all of these requirements has been identified, the process of drug development can continue. (wikipedia.org)
  • The review outlines the development of several promising drug candidates emphasizing the importance of each chemical scaffold. (spandidos-publications.com)
  • It has been formulated to be compatible with 96 or 384-well format polymerization assays such as in Biochem™ kits BK004 or BK011P or CytoDYNAMIX Screen™ BK004. (cytoskeleton.com)
  • In 2D culture, all cells can proliferate at a relatively constant rate in a planar space, and can be provided uniform access to nutrients, oxygen or drugs. (medsci.org)
  • After three adaptations, cells were cultured for 72 hours in an orthogonal experiment using drugs that were used for adaptation. (oncotarget.com)
  • The testosterone secretion from TM3 cells was measured using the enzyme-linked immunosorbent assay. (lookformedical.com)
  • It is known that the pathogenic properties of glioma cells and the response of glioma towards platinum-based drugs are strongly influenced by non-coding RNAs, particularly, by microRNAs (miRNAs) and long non-coding RNAs (lncRNAs). (eurekaselect.com)