• Inhibitors of topoisomerase II are important drugs used in the therapy of many neoplasms including breast cancer, lung cancer, testicular cancer, lymphomas and sarcomas. (ukessays.com)
  • Their in vitro antitumor activities against murine B16 melanoma and P388 leukemia cells were determined. (nih.gov)
  • 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. (biomedsearch.com)
  • 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. (biomedsearch.com)
  • 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. (biomedsearch.com)
  • 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. (biomedsearch.com)
  • We show that this assay detectsapoptosis in epithelial cells and that thesensitivity is sufficient for screening inthe 96-well format. (springer.com)
  • To date, the majority of the antiangiogenesis drug studies have been performed using endothelial cells isolated from either capillaries or large vessels. (ahajournals.org)
  • Brief heating of these drugs-treated cells at 65° for 10 min resulted in a rapid reduction in the number of protein/DNA complexes. (aspetjournals.org)
  • 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. (biomedcentral.com)
  • 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. (aacrjournals.org)
  • 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. (ddw-online.com)
  • 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. (ddw-online.com)
  • Also, many available human cells have not been very good at predicting side-effects of newly discovered drugs as they enter the pipeline. (ddw-online.com)
  • 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. (ddw-online.com)
  • 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. (ddw-online.com)
  • 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. (ddw-online.com)
  • 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. (ddw-online.com)
  • 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. (ddw-online.com)
  • 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). (ddw-online.com)
  • Depletion of CD8+ T-cells abrogated the antitumor response to the combination therapy. (nih.gov)
  • 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. (nih.gov)
  • Additive antitumor activity of dasatinib and Eto in MDA-MB-231 cells. (nih.gov)
  • 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. (biomedcentral.com)
  • The screen led to the identification of several compounds which were further selected for their preferential cytotoxicity towards acid-adapted cells. (biomedcentral.com)
  • Our study provides an example and a tool to identify anticancer drugs targeting acid-adapted cancer cells. (biomedcentral.com)
  • First of all, cancer cell line is extracted from the culture media and incubation of these cancer cells with tested drugs or compounds. (ukessays.com)
  • The gene expression and the drug resistance property of CD133 positive cancer stem cells, however, are still unknown. (springernature.com)
  • The toxicity of these Pt(II) complexes on noncancer cells was, in all cases, found to be reversed upon drug removal. (uc.pt)
  • 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. (nih.gov)
  • 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 . (aacrjournals.org)
  • The effects of valproic acid (VPA), an antiepileptic drug with histone deacetylase inhibitory activity, on mononuclear cells isolated from 40 CLL patients were evaluated. (uliege.be)
  • 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. (discoverx.com)
  • 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. (discoverx.com)
  • A ) From a whole-cell immunodetection assay, we selected 139 cell-permeable compounds that caused increases in phosphonucleolin staining in A549 cells ( 4 ). (sciencemag.org)
  • Furthermore, real-time analysis of the dynamic labeling assay for live/dead cells was investigated. (springer.com)
  • 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. (discoverx.com)
  • Bioassay-guided fractionations of the extract of Chaga mushrooms using a proliferation assay on human follicle dermal papilla cells (HFDPCs) gave five lanostane-type triterpenes (1-5), whose structures were identified by spectroscopic evidence. (tokushima-u.ac.jp)
  • however, stand-alone chemotherapy drugs suffer from numerous problems including rapid in vivo metabolism and/or excretion, inability to access and penetrate cancer cells, and nonspecific uptake by healthy cells and tissue. (hindawi.com)
  • Horizon's new platform enables researchers to study how new drugs are able to activate different types of immune cells as well as increase their ability to kill tumors. (labbulletin.com)
  • The in vitro assays revealed that two naphthalene diimide-polyamine conjugates could inhibit the growth of multiple cancer cell lines more potently than amonafide. (isharonline.org)
  • Larsson R, Nygren P: Pharmacological modification of multidrug resistance (MDR) in vitro detected by a novel fluorometric microculture cytotoxicity assay. (springer.com)
  • 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). (springer.com)
  • 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. (frontiersin.org)
  • 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. (exp-oncology.com.ua)
  • 15 16 17 18 19 The limited specificity of TST may result in unnecessary anti-tuberculosis treatment and the risk of significant drug toxicity. (bmj.com)
  • We previously designed a model to isolate pure populations of these CSCs from distinct solid tumors and used it to screen for molecules showing selective toxicity for this type of CSC. (ox.ac.uk)
  • These platforms such as organ-on-a-chip, biological scaffolding, or microdrop techniques offer substantial advantages in evaluating disease mechanisms, drug discovery, and toxicity testing and potentially, for tissue-replacement therapies. (genengnews.com)
  • Platinum based anticancer drugs induces normal tissue toxicity particularly to the kidneys and thus alternative metal compounds are presently being evaluated in clinical trials. (innovationinfo.org)
  • Characterization, chemical optimization and anti-tumour activity of a tubulin poison identified by a p53-based phenotypic screen. (biomedsearch.com)
  • 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. (intechopen.com)
  • 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. (ddw-online.com)
  • Phenotypic screening includes any screening where the molecular mechanism of action is not assumed and does not involve screening against an isolated target. (ddw-online.com)
  • Phenotypic assays share a common feature, ie there must be high confidence in their translation to human biology and disease. (ddw-online.com)
  • 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. (ddw-online.com)
  • 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. (ddw-online.com)
  • Profiling novel sulfonamide antitumor agents with cell-based phenotypic screens and array-based gene expression analysis. (naver.com)
  • Orlistat, or tetrahydrolipstatin (THL), is an FDA-approved antiobesity drug with potential antitumor activities. (nih.gov)
  • 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. (biomedsearch.com)
  • Burke JF, Duff PM, Pearson CK (1979) Effect of drugs on deoxyribonucleic acid synthesis in isolated mammalian cell nuclei. (springer.com)
  • This unique approach to controlled delivery in the brain should have a significant impact on treatment of glioblastoma multiforme and suggests previously undescribed routes for drug and gene delivery to treat other diseases of the central nervous system. (nih.gov)
  • Zebrafish represent a vertebrate model organism that has been widely, and increasingly, employed over the last decade in the study of developmental processes, wound healing, microbe-host interactions, and drug screening. (biomedcentral.com)
  • In recent years, there has been a growing interest in aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) because of their promising antineoplastic properties. (hindawi.com)
  • 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. (nih.gov)
  • 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). (nih.gov)
  • Assay for beta-Glucuronidase in Species of the Genus 'Escherichia' and Its Applications for Drinking-Water Analysis. (epa.gov)
  • Assay of Beta-Glucuronidase in Non-coli Escherichia Using EC-Mug Medium and the Colilert (Trade Name) System. (epa.gov)
  • Therapeutic Potential of Foldamers: From Chemical Biology Tools To Drug Candidates? (naver.com)
  • An ideal delivery system should be composed of biocompatible and biodegradable materials, reproducibly assemble into the desired size range, encapsulate a wide range of drugs and drug classes, maintain particle size in biological media, have the ability to attach cell-specific targeting groups, and release the therapeutic at the site of disease. (hindawi.com)
  • Drugs activating BK channels therefore bear substantial therapeutic potential, but their deployment has been hindered in part because the mode of action remains obscure. (uef.fi)
  • We identified several agents (from Food and Drug Administration-approved products) that potently inhibit proliferation and self-renewal of BCSCs. (nih.gov)
  • The platform allows researchers to test thousands of new immuno-oncology drugs simultaneously, alone or in combination with other drugs. (labbulletin.com)
  • Horizon's new immuno-oncology research platform will be deployed to support this effort as well as being offered commercially as a set of assay services to clients. (labbulletin.com)
  • Tewey KM, Chen GL, Nelson EM, Liu LF: Intercalative antitumor drugs interfere with the breakage-reunion reaction of mammalian DNA topoisomerase II. (springer.com)
  • New saintopin-type antibiotics (e.g., saintopin, saintopin E, UCE1022, UCE6) with a naphthacene-dione structure have been discovered through our mechanistically oriented screening using purified mammalian DNA topoisomerases. (aspetjournals.org)
  • 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). (aacrjournals.org)
  • Here, we present data for several new PathHunter® Checkpoint assays that target clinically relevant co-inhibitory and co-stimulatory checkpoint receptors using the industry-validated Enzyme Fragment Complementation (EFC) technology. (discoverx.com)