Lethality assayCytotoxicityChemotherapyProteinsPreclinicalEvaluationGrowth inhibitionPotentVitroAntibodiesCompoundsSynthesisToxicityDiscoveryAntimicrobialAnalyticalDiagnosticSensitivityMoleculesHigh throughputMicrotubuleDiseaseDPPHPROFILESMedicinal chemistryBioactiveAnticancer drugActivityPotentialProteinWidespreadPatient'sResistance2021ApproachesPeptidesLibrariesTargetsCharacterizationClinicalDerivativesInhibitorsSyntheticDevelopmentMolecularCellCancerRESULTSStudiesExperimentalTumorInvestigationsPropertiesExposureEffectsSignificantMaterialNaturalUniversityWidelyAnalysisLargeLeukemia cellsOpportunities
Lethality assay5
- 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)
- The same extracts were assessed for their antioxidative potentials with the use of DPPH free radical scavenging assay followed by determination of HRBC membrane stabilization method, Brine Shrimp Lethality Assay (BSLA) and GC-MS analysis. (biomedcentral.com)
- During Brine Shrimp Lethality Assay, all extracts of BG were found to be bioactive and the degree of lethality was found to be concentration dependent. (biomedcentral.com)
- The Brine Shrimp Lethality Assay found extracts to be bioactive suggesting extracts as a promising candidate for plant-derived anti-tumor compounds. (biomedcentral.com)
- The ethanolic extracts of the plant were examined for the presence of bioactive components and their total flavonoid content, with focusing on quercetin detection using thin layer bioautography (TLB) and brine shrimp lethality assay (BSLA) for cytotoxicity. (who.int)
Cytotoxicity5
- The negative results for cytotoxic and antimicrobial assays indicated possible low cytotoxicity to the extract. (researchgate.net)
- Biological assays to test the cytotoxicity of the compound 1b combined with electroporation were performed to determine its potential for future medical applications in cancer treatment. (hindawi.com)
- It has been proven that combining electroporation with chemotherapy potentiates the cytotoxicity of drugs when the drugs' efficacy is limited by its uptake in the cell [ 9 - 13 ]. (hindawi.com)
- The search for targeted drugs for cancer treatment includes consideration of natural products, which may provide new opportunities for antitumor cytotoxicity as single agents or in combination therapy. (cancer.gov)
- This assay has been extensively used for different studies such as for preliminary toxicity screening of plant extracts, detection of fungal toxins, plant extract toxicity, heavy metals, cyanobacteria toxins, pesticides, and cytotoxicity testing of dental materials [ 9 ]. (biomedcentral.com)
Chemotherapy4
- The aim is to try to identify drugs that may be effective in killing leukemia cells for those patients who will not be cured with conventional chemotherapy. (clincosm.com)
- The concept has now been extended to embrace synthetic lethal drug sensitivity, such as that observed with PARP inhibitors in combination with DNA-damaging chemotherapy in a variety of BRCA defective tumors 10 . (nature.com)
- The major concern of chemotherapy is the side effects of existing drugs ( Baldo and Pham, 2013 ). (japsonline.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)
Proteins3
- Protein binding assays assesses the degree to which drugs attaches to proteins within the plasma/tissue. (td2inc.com)
- Their analysis is critical to determining the therapeutic proteins that will fail to induce immune responses while still performing their biological function. (genengnews.com)
- Compounds of interest include not only classical "drug-like" organic small molecules, but also peptides, proteins, and other bioactive chemical classes. (cancer.gov)
Preclinical1
- 50 years of preclinical anticancer drug screening:empirical to target-driven approaches. (jscimedcentral.com)
Evaluation2
- Screening tools for the evaluation of a drug's ability to cross various biological membrane systems in a microplate format. (td2inc.com)
- Our medicinal chemistry program involves the development, synthesis, and biological evaluation of antibacterial agents derived from naturally occurring molecules. (unca.edu)
Growth inhibition3
- 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)
- Triticum aestivum L. root growth inhibition test and Allium cepa L. assay were used to assess the cytotoxic potential of phosphonates. (japsonline.com)
Potent2
- Here, we generate dromedary camel nanobodies targeting B7-H3 and demonstrate that CAR-T cells, based on the nanobodies recognizing the IgC but not IgV domain, had potent antitumour activity against large tumors in female mice. (nature.com)
- Potent cell growth inhibitory properties were shown by ligands MS47 and MS49 against human melanoma MDA-MB-435, colon cancer HCT-116 and COLO 205, and pancreatic cancer MIA PaCa-2 cell lines, as evidenced by MTT assay. (openmedicinalchemistryjournal.com)
Vitro2
- Lenis-Rojas OA, Cordeiro S, Horta-Meireles M, Fern?ndez JAA, Fern?ndez Vila S, Rubiolo JA, Cabezas-Sainz P, Sanchez L, Fernandes AR, Royo B. N-Heterocyclic Carbene Iron Complexes as Anticancer Agents: In Vitro and In Vivo Biological Studies. (ucdenver.edu)
- In vitro drug metabolism studies, are a screening mechanism to characterize drug metabolites, elucidate their pathways, to help with further in vivo testing. (td2inc.com)
Antibodies1
- While the epitope of most B7-H3 antibodies has not been described, one of the clinically tested antitumor antibodies (8H9) was found to bind to the IgV domain 19 . (nature.com)
Compounds4
- Therefore, a rationale for treating hypertension would be to administer drugs or natural compounds which selectively inhibit ACE. (scielo.br)
- O. Nagaraja, Y.D. Bodke, I. Pushpavathi, S. Ravi Kumar, Synthesis, characterization and biological investigations of potentially bioactive heterocyclic compounds containing 4-hydroxy coumarin. (dntb.gov.ua)
- The GC-MS analysis of the methanolic extract of BG revealed 23 compounds which are reported to possess different biological activities. (biomedcentral.com)
- Studies have found very good relationship between this simple, inexpensive, and bench-top assay and the antitumor potential of the cytotoxic compounds [ 10 ]. (biomedcentral.com)
Synthesis5
- This one-day conference held on 1 July 2008, and sponsored by SCI, the RSC, and ICI brought together scientists from the Republic of Ireland and from Northern Ireland who have varied interests in drug discovery and development and a common interest in synthesis. (soci.org)
- Professor Maguire underlined the central importance of organic synthesis to the field of chemical biology and the interfaces with drug development and process development. (soci.org)
- Of course, clandestine synthesis of ecstasy and other drugs of abuse is widespread. (soci.org)
- Stevenson's talk reminded us that in many cases de novo synthesis of natural products is the only way to obtain sufficient quantities to permit their full structural characterisation and study in detail their biological activity. (soci.org)
- O. Nagaraja, Y.D. Bodke, R. Kenchappa, S. Ravi Kumar, Synthesis and characterization of 3-[3-(1H-benzimidazol-2-ylsulfanyl)-3-phenyl propanoyl]-2H-chromen-2-one derivatives as potential biological agents. (dntb.gov.ua)
Toxicity3
- Its low toxicity, high efficiency, and controllable drug release advantages make it have good application effects. (frontiersin.org)
- The development of platinum-drug resistance in cancer patients, the general toxicity and severe side effects of platinum drugs however required a different approach in the research of anticancer metal complexes [ 2 ]. (hindawi.com)
- Human-derived hepatic cell lines are a valuable alternative to primary hepatocytes for drug metabolism, transport and toxicity studies. (cancerindex.org)
Discovery15
- Mechanism-based target identification and drug discovery in cancer research. (jscimedcentral.com)
- Drug repositioning and pharmacophore identification in the discovery of hookworm MIF inhibitors. (jscimedcentral.com)
- Organic chemistry in drug discovery. (jscimedcentral.com)
- The role of the medicinal chemist in drug discovery--then and now. (jscimedcentral.com)
- 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)
- TL238) for anti-tubulin ligand drug discovery. (cytoskeleton.com)
- Wolfe, A. L. Advances in antibiotic drug discovery: Reducing the barriers for antibiotic development" Future Medicinal Chemistry 2020 , 12(22) , 2067-2087. (unca.edu)
- The Molecular Targets Program (MTP) provides the focus and infrastructure that enables CCR investigators to pursue molecularly targeted drug discovery research by promoting an interdisciplinary, collaborative, team-oriented approach to identifying and validating potential cancer-pertinent targets. (cancer.gov)
- Since the advent of molecular cloning, target based screening has become the norm in pharmaceutical drug discovery. (docksci.com)
- issues that often frustrate the present target based drug discovery programs. (docksci.com)
- 2012). However, many drug discovery efforts rely on screening to identify starting points for Medicinal Chemistry, and screening in vivo in most cases is not commercially or ethically viable. (docksci.com)
- In order to limit the reliance on non-predictive animal models, screening strategies utilizing human pluripotent stem cells (hPSCs) are increasingly considered as resources for drug discovery. (docksci.com)
- In the early phases of drug discovery, phenotypic assays can be used to further our knowledge of the disease process and to identify those end points that are most likely to translate to the clinic. (docksci.com)
- The perspective by Dr. Swinney analyzes the phenotypic end points used in the discovery of new molecular entities that have resulted from phenotypic drug discovery efforts. (docksci.com)
- 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)
Antimicrobial1
- Several NTM strains are resistant to many antimicrobial drugs, making treatment difficult ( 3 ). (cdc.gov)
Analytical2
- Professor Anita Maguire opened the conference with an introduction to the venue, The Analytical and Biological Chemistry Research Facility, University College Cork, which brings together researchers from the fields of analytical and biological chemistry and is currently hosting a new programme of undergraduate research. (soci.org)
- Hence, relatively straightforward analytical detection of this pyridine can instantly link, or not, a particular batch of drug to a particular clandestine production facility. (soci.org)
Diagnostic1
- 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)
Sensitivity4
- This clinical trial uses a laboratory test called a high throughput sensitivity assay in planning treatment for patients with relapsed or refractory acute myeloid leukemia. (clincosm.com)
- To obtain results from a high throughput drug sensitivity assay within 10 days, procure drug within 14 days and initiate treatment within 21 days. (clincosm.com)
- A patient receives a drug intervention based on the results of a high throughput sensitivity assay. (clincosm.com)
- Patients receive 1 of 160 possible interventions based on high throughput drug sensitivity assay. (clincosm.com)
Molecules2
- Typically, low molecular weight drugs are not recognized by the immune system, whereas protein molecules of much higher molecular weight invariably are. (genengnews.com)
- A large number of potential drug targets have been cloned and functionally expressed, and enormous progress has been made in the development, miniaturization and automation of cell based assays on target molecules recombinantly expressed in mammalian cell lines. (docksci.com)
High throughput3
- Whether treatment was administered in the time frame based on the high throughput drug screen. (clincosm.com)
- Development of a Robust and Quantitative High Throughput Screening Method for Antibiotic Production in Bacterial Libraries. (unca.edu)
- In this case, phenotypic screening relies on an appropriate tissueor cell-based assay that can be miniaturized and used in combination with high throughput tools. (docksci.com)
Microtubule1
- Microtubule binding drugs are of special interest as they have important roles in the modulation of cellular functions and many of them act as anticancer agents. (rgcb.res.in)
Disease5
- This review presents the molecular mechanisms supporting the use of HER2-targeted drugs in combination with immunotherapy and provides an overview of the therapeutic scenario of HER2-positive disease. (bvsalud.org)
- The goal is to use this laboratory assay to best match a drug to a patient's disease. (clincosm.com)
- This assay best matches a drug to the patient's disease. (clincosm.com)
- There is still no drug that alters the state of the disease. (helsinki.fi)
- If ER stress is a significant factor that affects the disease development, it would be important to find a drug that alters these mechanisms and UPR. (helsinki.fi)
DPPH1
- SOR), hydrogen peroxide, and 2, 2-Diphenyl-2-picrylhydrazyl (DPPH) radical activity by a model (most biological y active) of the anticancer plant was also evaluated. (who.int)
PROFILES2
- Below are the most recent publications written about "Drug Screening Assays, Antitumor" by people in Profiles. (ucdenver.edu)
- Keating's programme aims to elucidate full impurity profiles for drugs in relation to the full synthetic pathway employed. (soci.org)
Medicinal chemistry1
- Screening in vivo may be feasible, if a good starting point for Medicinal Chemistry and a clear strategy for differentiation exist. (docksci.com)
Bioactive1
- M. Gaba, C. Mohan, Development of drugs based on imidazole and benzimidazole bioactive heterocycles: recent advances and future directions. (dntb.gov.ua)
Anticancer drug1
- The contribution of synthetic organic chemistry to anticancer drug development. (jscimedcentral.com)
Activity7
- To confirm this popular use, ethanol extract from leaves of G. globosa L. was prepared by maceration and analyzed by some phytochemical and biological assays, including cardiovascular activity. (researchgate.net)
- The biological activity of HTS02 is assessed by a tubulin polymerization assay. (cytoskeleton.com)
- In the lab we systematically derivatize each targets core structure to improve both their antibacterial activity and their physical properties in order to make them a viable drug molecule. (unca.edu)
- Pharmacophore-based activity profiling screen demonstrated some biological targets that MS44-53 may modulate their biological response, and thus can be considered as potential drugs to treat different kinds of diseases, such as carcinoma, diabetes type II, bacterial infection and cardiovascular diseases. (openmedicinalchemistryjournal.com)
- 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)
- NSAIDS are widely used for their anti-inflammatory, analgesic and antipyretic activity and are among the most widely used drugs worldwide [ 6 ]. (biomedcentral.com)
- It is well known that biological activity depends on the chemical structure ( Lichota and Gwozdzinski, 2018 ). (japsonline.com)
Potential7
- Sawa M, Masai H. Drug design with Cdc7 kinase: a potential novel cancer therapy target. (jscimedcentral.com)
- Emerging evidence suggests that they provide a cellular mechanism for induction and emergence of drug resistance and contribute to increased invasive and metastatic potential. (frontiersin.org)
- Drug delivery systems seem to be a new method for improving drug targeting and release into cells, bringing new opportunities for improving drug efficiency and avoiding potential side effects. (frontiersin.org)
- This symposium presents a remarkable opportunity to convene with other researchers, clinicians, and industry leaders to discuss the extraordinary progress and immense potential of new drug therapies and technologies in paving the way for a brighter future in cancer treatment. (nyas.org)
- discusses the potential for using zebrafish as a model system, enabling large scale behavior based screens for central nervous system disorders. (docksci.com)
- Introduction The research of Hatch (1) has greatly increased our understand- ing of the use and potential limitations of biological markers for adverse reproductive effects. (cdc.gov)
- Exposure to a potential fetal health hazard can be estimated through ecological assessment (e.g., testing the community water supply), questionnaires (e.g., classifying residents accord- ing to whether they drink bottled or tap water), or biological markers (e.g., testing for exposures to chemicals or solvents found in tap water). (cdc.gov)
Protein3
- Protein quantitation was performed using the Pr ecision Red Protein Assay Reagent (Cat. (cytoskeleton.com)
- An ASSAY UNIT is defined as the amount of HTS02 protein needed to achieve a tubulin polymerization signal of OD340 of 0.1 - 0.15 in 30 minutes at 37°C in G-PEM buffer. (cytoskeleton.com)
- The protein concentration for HTS02 in this assay is approximately 4 mg/ml. (cytoskeleton.com)
Widespread1
- However, several hurdles need to be overcome before widespread implementation of hPSC-based assays. (docksci.com)
Patient's2
- This assay will test multiple drugs simultaneously against a patient's own donated blood sample. (clincosm.com)
- In oncology, mouse xenograft models, based on a patient's tumor cells, have been used to select between drugs (Wu et al. (docksci.com)
Resistance1
- This low survival may result from the metastasis of cancer cells and arising resistance to drugs. (oncotarget.com)
20211
- Mar Drugs 19: 361, 2021. (cancer.gov)
Approaches3
- Target based screening is likely to provide very good drug candidates for monogenic diseases, and the following collection of manuscripts is not meant to discourage the use of target based approaches. (docksci.com)
- Here, target agnostic approaches using phenotypic assays may offer significant benefit. (docksci.com)
- Viswanathan and colleagues reviewed the recent progress in the culture of hPSCs with emphasis on the importance of the environment surrounding these cells and high content analysis approaches for assay development. (docksci.com)
Peptides1
- These include EpiScreen™, a T-cell epitope mapping technology that screens peptides for their immunostimulatory properties, and EpiScreen DC:T cell assay, which screens biologics for their immunogenicity. (genengnews.com)
Libraries1
- The limited throughput of phenotypic assays compared to most target-based assays necessitates smaller libraries that are optimized with regard to biological and chemical diversity. (docksci.com)
Targets2
- Billingsley ML. Druggable targets and targeted drugs: enhancing the development of new therapeutics. (jscimedcentral.com)
- Most of these drugs interact relatively weakly with a number of targets, and the complete profile of their molecular interactions is not well-known. (docksci.com)
Characterization1
- Experimental analysis was also conducted on the characterization ability, drug release, and targeted therapy of nanomedicine. (frontiersin.org)
Clinical4
- Additionally, the irruption of antibody-drug conjugates and other novel HER2-targeted agents has led to the development of numerous clinical trials showing promising results. (bvsalud.org)
- However, despite growing biological and clinical significance, little is known about the structural arrangement of this receptor or any of its family members. (uci.edu)
- This approach has delivered many clinical candidates but relatively few new drugs. (docksci.com)
- Here, we report the draft genomes for 45 Enterobacterales clinical isolates, including historical and contemporary drug-resistant organisms, obtained in Pakistan between 1998 and 2016: 5 Serratia, 3 Salmonella, 3 Enterobacter, and 34 Klebsiella. (cdc.gov)
Derivatives1
- We will also evaluate our derivatives in house using an antibacterial assay. (unca.edu)
Inhibitors2
- Methods of investigating the effectiveness of anticancer cytotoxic drugs and biologic inhibitors. (ucdenver.edu)
- Tubulin polymerization must also be responsive to polymerization enhancers (paclitaxel) and inhibitors (nocodazole) at 5 µM drug concentration. (cytoskeleton.com)
Synthetic1
- The clandestine chemist has to switch their method of production according to the availability of different starting materials, thus a number of synthetic routes are available to a given drug molecule. (soci.org)
Development5
- Therefore, Src has been considered a target molecule for drug development. (oncotarget.com)
- These findings will assist the development of anti-tumour drugs to treat lung cancer. (oncotarget.com)
- Characterisation of ER stress in PD models may be important for the current and future drug development of PD. (helsinki.fi)
- The development of bioinformatics technology has enabled nanomedicine to play a significant role in drug delivery systems. (frontiersin.org)
- I develop my courses with a focus on application (biological, environmental, material etc.) and technology development. (unca.edu)
Molecular2
- Guidebook on molecular modeling in drug design: Academic Press. (jscimedcentral.com)
- Ooms F. Molecular modeling and computer aided drug design. (jscimedcentral.com)
Cell2
- 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)
- Promising examples include anti-microbial assays, cell proliferation, platelet aggregation, and insulin release from pancreatic β-cells. (docksci.com)
Cancer2
- Li X, Taratula O, Taratula O, Schumann C, Minko T. LHRH-Targeted Drug Delivery Systems for Cancer Therapy. (jscimedcentral.com)
- Targeted therapy uses targeted drugs to maintain a high concentration of the drug in the tumor area, improving the killing efficiency of cancer cells while avoiding damage to other normal cells. (frontiersin.org)
RESULTS3
- RESULTS: 7780 abstracts were screened, identifying 45 publications with 208 patients, corresponding to 275 lines of HER2-targeted therapy for BC LM which met inclusion criteria. (bvsalud.org)
- Time from sample procurement to assay results. (clincosm.com)
- Example of Caco-2 Assay results. (td2inc.com)
Studies1
- However, with an adeq battery of necf expsre blmarkers, prospective studies of en- vironmental effects on pregnancy outcomes might be possible. (cdc.gov)
Experimental1
- Therefore, based on the characteristics of black phosphorus two-dimensional nanomedicine, experimental designs were conducted on its nanosheet preparation, polyethylene glycol modification, and anti-tumor drug loading. (frontiersin.org)
Tumor2
- Moreover, common targeted therapeutic drug formulations have weak stability in malignant tumor leukemia, and their application effects are limited. (frontiersin.org)
- Its drug release characteristics perform well in photothermal therapy, indicating that black phosphorus nano drugs can improve the biological safety and applicability of drugs in new tumor targeted therapy. (frontiersin.org)
Investigations1
- However, their relevance for investigations of drug-drug and drug-organic anion (e.g., bile acid, steroid hormone) interactions at the transporter level remains to be established. (cancerindex.org)
Properties1
- Various anti-oxidants have found to possess properties such as anti-atherosclerotic, antitumor, anti-mutagenic, anti-carcinogenic to name a few selected ones [ 4 ]. (biomedcentral.com)
Exposure2
Effects1
- The first-in-human testing of scFv-based B7-H3 CAR-T cells has shown antitumor response against anaplastic meningioma and childhood diffuse intrinsic pontine glioma without severe side effects 16 , 17 . (nature.com)
Significant1
- Since the clandestine chemist is unlikely to engage in rigorous purification of their products, most drugs of abuse contain significant impurities. (soci.org)
Material1
- 1979. Quantitative trace analysis of thallium in biological material. (cdc.gov)
Natural1
- Some aspects of recent research with natural products directed to produce anti-hypertensive drugs are discussed. (scielo.br)
University1
- Dr J J Keating (University College Cork) is one of a small group of chemists who synthesise drugs of abuse such as, for example, MDMA (more commonly known as ecstasy) and want the world to know about it! (soci.org)
Widely1
- To date, such biological markers have not been widely available nor have they been widely used when they are available. (cdc.gov)
Analysis2
- TD2 has validated this assay using the Rapid Equilibrium Device and analysis done by LC-MS. (td2inc.com)
- In: Analysis of hazardous substances in biological materials. (cdc.gov)
Large2
- Cathepsin K, a member of a large family of cysteine peptidases, is an enzyme that breaks down the collagen bone matrix as part of a normal biological process. (bioworld.com)
- As urinary screens, they are noninvasve and apble on a large scale with current labo techniques For short-term esue, glucaric acid, thloetbers, and mug tests are usefl. (cdc.gov)
Leukemia cells1
- The two-dimensional nano drug carrier has high safety and effectiveness in drug delivery, and its targeted treatment effect on acute T lymphoblastic leukemia cells is obvious. (frontiersin.org)
Opportunities1
- This may be of concern to the user, but Keating is most interested in the opportunities this gives for forensic linkage of recovered drugs to their production site. (soci.org)