منابع مشابه
A quantitative systems pharmacology analysis of KRAS G12C covalent inhibitors
The KRAS oncogene is the most common, activating, oncogenic mutation in human cancer. KRAS has proven difficult to target effectively. Two different strategies have recently been described for covalently targeting the most common activating KRAS mutant in lung cancer, KRAS G12C. Previously, we have developed a computational model of the processes that regulate Ras activation and this model has ...
متن کاملPotent and Selective Covalent Quinazoline Inhibitors of KRAS G12C.
Targeted covalent small molecules have shown promise for cancers driven by KRAS G12C. Allosteric compounds that access an inducible pocket formed by movement of a dynamic structural element in KRAS, switch II, have been reported, but these compounds require further optimization to enable their advancement into clinical development. We demonstrate that covalent quinazoline-based switch II pocket...
متن کاملQuantitative Systems Pharmacology Analysis of KRAS G12C Covalent Inhibitors.
KRAS has proven difficult to target pharmacologically. Two strategies have recently been described for covalently targeting the most common KRAS mutant in lung cancer, KRAS G12C. Previously, we developed a computational model of the processes that regulate Ras activation. Here, we use this model to investigate KRAS G12C covalent inhibitors. We updated the model to include Ras protein turnover, ...
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The contributions from Biacore technology continue to have a widening impact on all aspects of the drug discovery process in today’s pharmaceutical industry. As biosensor technology became a practical reality in the laboratory during the early 1990s, it was readily accepted by the scientific community as a powerful analytical technique for evaluating the kinetic parameters of molecular interact...
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T here aren't many sports articles in the journal Science, so it was with great interest that I read " A Late Hit for Pro-Football Players " by Greg Miller (www. sciencemag.org). 3 This article is a very interesting compilation of recent research and developments in the area of sports-related concussion. The article highlights the efforts of Chris Nowinski, a former Harvard football standout wh...
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ژورنال
عنوان ژورنال: Science-Business eXchange
سال: 2014
ISSN: 1945-3477
DOI: 10.1038/scibx.2014.3