Streptomyces lavendulae
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. ... Many natural compounds have led to the discovery of drugs used to treat human disease. Out of the 22,500 biologically active ... Research on Antibiotic Screening in Japan over the Last Decade: A Producing Microorganisms Approach. Actinomycetologica. 9:100- ...
Zidovudine
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 ... Drugs with non-standard legal status, Articles with changed EBI identifier, ECHA InfoCard ID from Wikidata, Drug has EMA link, ... leading to the development of the antitumor agent 6-mercaptopurine. Richard E. Beltz first synthesized AZT in 1961, but did not ... This assay could simultaneously test both the anti-HIV effect of the compounds and their toxicity against infected T cells. In ...
MTOR inhibitors
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 ...
Ulcerative colitis
October 2019). "Performance of Interferon-Gamma Release Assays for Tuberculosis Screening in Pediatric Inflammatory Bowel ... Many 5-ASA drugs have been developed with the aim of delivering the active compound to the large intestine to maintain ... Food and Drug Administration. Dignass AU, Gasche C, Bettenworth D, Birgegård G, Danese S, Gisbert JP, et al. (March 2015). " ... July 2018). "A Prospective Study to Monitor for Tuberculosis During Anti-tumour Necrosis Factor Therapy in Patients With ...
Hartmann F. Stähelin
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 ...
Folate targeting
2007). "Preclinical antitumor activity of a novel folate-targeted dual drug conjugate". Mol. Pharm. 4 (5): 659-67. doi:10.1021/ ... Leamon CP (December 2008). "Folate-targeted drug strategies for the treatment of cancer". Curr Opin Investig Drugs. 9 (12): ... 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 ...
Camptothecin
It was discovered in 1966 by M. E. Wall and M. C. Wani in systematic screening of natural products for anticancer drugs. It was ... Reduced drug-HSA interactions could result in improved activity. Studies have shown that substitution at position 7, 9, 10 and ... The C- and D-rings have an essential role in the antitumor activity. Replacement in any position results in much less potent ... compound than parent compound in other cytotoxicity assay. The E-ring doesn't allow many structural changes without losing CPT ...
Ligand binding assay
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 ... pharmacologists utilize assays in order to create drugs that are selective, or mimic, the endogenously found cellular ... 2009). Ligand-binding assays development, validation, and implementation in the drug development arena. Hoboken, N.J.: John ...
Organ-on-a-chip
"Such cell cultures can lead to new insights into cell and organ function and be used for drug screening". A kidney-on-a-chip ... It allows patients, especially out-patients, to self-serve the drugs with minimal possibility of experiencing acute drug ... October 2018). "Live-cell phenotypic-biomarker microfluidic assay for the risk stratification of cancer patients via machine ... based biomimetic liver tumor-on-a-chip proved to be a suitable design for further anti-tumor studies. Zhou et al. analyzed ...
Discovery and development of antiandrogens
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 ... In 1989 the United States Food and Drug Administration (FDA) approved it for use the treatment of prostate cancer. In 1995, ...
Kinesin-like protein KIF11
"In vitro screening for inhibitors of the human mitotic kinesin Eg5 with antimitotic and antitumor activities". Mol Cancer Ther ... microtubule gliding assays, single molecule motility assays, and optical trap assays. In microtubule gliding assays, kinesins ... Drugs that specifically inhibit only human Kinesin-5 are alternatives to the taxanes and vinc alkaloids that target ... The majority of human Kinesin-5 inhibitors are selective, because they bind to a drug 'hot spot', composed of residues from the ...
Drug discovery
... drugs). Other methods, such as virtual high throughput screening, where screening is done using computer-generated models and ... 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 ... It is unlikely that a perfect drug candidate will emerge from these early screening runs. One of the first steps is to screen ...
DNA polymerase beta
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 ... "Overexpression of DNA polymerase beta in cell results in a mutator phenotype and a decreased sensitivity to anticancer drugs". ...
RNA therapeutics
... rationale and design of screening assays, and the application of such assays for screening of natural product extracts and the ... Sahin U, Karikó K, Türeci Ö (October 2014). "mRNA-based therapeutics--developing a new class of drugs". Nature Reviews. Drug ... SLR14 improved antitumor efficacy of anti-PD1 antibody over single-agent treatment. SLR14 was absorbed by CD11b+ myeloid cells ... Antisense drugs are based on the fact that antisense RNA hybridizes with and inactivates mRNA. These drugs are short sequences ...
Microvesicle
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 have been implicated in numerous physiologic processes, including anti-tumor effects, tumor immune ...
Cancer research
Can it be a Multifunctional Drug?". Current Drug Metabolism. 21 (7): 512-524. doi:10.2174/1389200221666200610172105. PMID ... Some screening protocols are currently not accurate (such as prostate-specific antigen testing). Others such as a colonoscopy ... "Gene Therapy, Cancer-Killing Viruses And New Drugs Highlight Novel Approaches To Cancer Treatment". Medical News Today. ... are assayed on cultures of bacteria and mammalian cells. The goal of oncogenomics is to identify new oncogenes or tumor ...
Natural product
Drug Discovery - Is Mother Nature still the number one source for promising new drugs? Patrick GL (2013). "12.4.2: Medical ... 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 ...
Flutamide
Boelsterli UA, Ho HK, Zhou S, Leow KY (October 2006). "Bioactivation and hepatotoxicity of nitroaromatic drugs". Current Drug ... February 2004). "Comparison of the Hershberger assay and androgen receptor binding assay of twelve chemicals". Toxicology. 195 ... "Effects of combined treatment with niftolide and low doses of antitumor estrogen preparation, chlorotrianizene, on rat prostate ... evidence for complex I inhibition and mitochondrial dysfunction using toxicogenomic screening". Chemical Research in Toxicology ...
Paclitaxel
Drugs with non-standard legal status, Articles with changed EBI identifier, ECHA InfoCard ID from Wikidata, Drug has EMA link, ... 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 ...
Cyclin-dependent kinase 5
Cdk5 has been proven to be directly linked with drug abuse. We know that drugs act in the reward system, reaching their action ... Quintavalle M, Elia L, Price JH, Heynen-Genel S, Courtneidge SA (July 2011). "A cell-based high-content screening assay reveals ... 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. ...
Isothermal microcalorimetry
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 ... For example, IMC has been widely used for many years in shelf life studies of solid drug formulations in the pharmaceutical ... This is especially useful for comparative screening-e.g. the effects of different combinations of material composition and/or ...
Chemotherapy
The first chemotherapy drug to be developed from this line of research was mustine. Since then, many other drugs have been ... 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 ...
Induced stem cells
... and drug screening applications. Using MitoBloCK-6 and/or PluriSIn # 1 the differentiated progenitor cells can be further ... of drugs, and toxicity testing of various drugs. The tissue grown from iPSCs, placed in the "chimeric" embryos in the early ... 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/ ...
Survivin
... 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 ... They found that cells halted in S phase were significantly more sensitive to the cytotoxic effects of the drugs. To determine ... "Survivin-derived peptide epitopes and their role for induction of antitumor immunity in hematological malignancies". Leuk. ...
Bafilomycin
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 human lung cancer samples, V-ATPase expression was correlated with drug resistance. A large number of V-ATPase subunit ... In a rabbit contractility assay, bafilomycin was used to pre-treat isolated rabbit aorta. The lipophilic agent xylometazoline, ...
Vaccine
Drugs Controller General of India is the head of department of the Central Drugs Standard Control Organization of the ... Pregnant women are often screened for continued resistance to rubella. The human papillomavirus vaccine is recommended in the U ... "Vaccine product approval process". U.S. Food and Drug Administration (FDA). 30 January 2020. Archived from the original on 27 ... van Oirschot JT, Gielkens AL, Moormann RJ, Berns AJ (June 1990). "Marker vaccines, virus protein-specific antibody assays and ...
Structural Genomics Consortium
... is modelled after the non-profit drug research and development Drugs for Neglected Diseases Initiative (DNDi). READDI™ and VIMI ... The SGC initiated a concerted effort to develop disease-relevant, cell-based assays using (primary) cells or tissue from ... Patient-derived cell lines are screened against chemical modulators (including chemical probes and chemogenomic compounds) with ... with Antitumor Activity". ACS Medicinal Chemistry Letters. 9 (7): 612-617. doi:10.1021/acsmedchemlett.8b00014. ISSN 1948-5875. ...
C-Met inhibitor
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. (CS1 ... Still, the risk of accumulated toxicity and interactions with other drugs remains. In 2011 PF-02341066 (now named crizotinib) ... "The discovery of benzanilides as c-Met receptor tyrosine kinase inhibitors by a directed screening approach", Bioorganic & ...
Platinum nanoparticle
In another study, a Pt nanoparticle of diameter 140 nm was encapsulated within a PEG nanoparticle to move an antitumor drug, ... The damage to the DNA was measured for individual cells using single-gel electrophoresis via the comet assay. Researchers have ... and anticancer drugs. These applications utilize platinum nanomaterials due to their catalytic ability to oxidize CO and NOx, ... Optical Screening Method for Discovery of Better Electrocatalysts" (PDF). Science. 280 (5370): 1735-7. Bibcode:1998Sci... ...
N-Acylethanolamine
... and inspired by US drug policy called The Fight against Drugs, with introduction of better fence systems, more sniffer-dogs, ... For severely injured trauma patients with Injury Severity Score ≥16, a THC(+) screen show significantly lower intensive care ... is why cannabinoids are found to be selective antitumour compounds, that can kill tumour cells, by growth arrest or apoptosis, ... of which several demonstrating significantly different expression in the tissues assayed, demonstrate the diversity of lipid ...