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sos signal timing

An orthosteric inhibitor of the Ras-Sos interaction, Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices, Small molecule binding sites on the Ras:SOS complex can be exploited for inhibition of Ras activation, Rational design of small molecule inhibitors targeting the Ras GEF, SOS1, High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling, Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange, Small molecule-mediated activation of RAS elicits biphasic modulation of phospho-ERK levels that are regulated through negative feedback on SOS1, Structural snapshots of the mechanism and inhibition of a guanine nucleotide exchange factor, Structural and functional analysis of a mutant Ras protein that is insensitive to nitric oxide activation, The structural basis of the activation of Ras by Sos, Structural evidence for feedback activation by Ras.GTP of the Ras-specific nucleotide exchange factor SOS, Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation, A Ras-induced conformational switch in the Ras activator Son of sevenless, Mammalian son of sevenless guanine nucleotide exchange factors: Old concepts and new perspectives, Novel substituted quinazolines for potent EGFR tyrosine kinase inhibitors, Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor, Identification and characterization of essential genes in the human genome, Overview of the CCP4 suite and current developments, REFMAC5 for the refinement of macromolecular crystal structures, PRODRG: A tool for high-throughput crystallography of protein-ligand complexes, Drug combination studies and their synergy quantification using the Chou-Talalay method, Proceedings of the National Academy of Sciences, Earth, Atmospheric, and Planetary Sciences,, Creative Commons Attribution-NonCommercial-NoDerivatives License 4.0 (CC BY-NC-ND), Opinion: A risk–benefit framework for human research during the COVID-19 pandemic, Core Concept: The pandemic is prompting widespread use—and misuse—of real-world data, Volcanic eruption’s effects on Roman Republic. Fragment F1 was therefore chosen as the starting point for optimization (see also SI Appendix, Supplementary Results for further details on the fragment hit prioritization and fragment binding modes). Models were rebuilt using Coot (40) and refined using REFMAC (41). Copyright © 2019 the Author(s). (30). This is similar to recombination-dependent adaptive mutation (studied here), but the two mutation routes have some different genetic requirements (reviewed by ref. Launch Settings from your Home screen. Combination of both approaches was essential and led to the design of compounds addressing this subpocket, with an improved IC50 of 21 nM. Published by PNAS. We could demonstrate that selective inhibition of SOS1 effectively down-regulates the levels of active RAS in tumor cells. During the peak period, record the average lengths of the various signal We selected NCI-H358 cells, which are heterozygous for KRASG12C, and treated them with a combination of the covalent KRASG12C inhibitor ARS-853 and either compound 23 or 24.

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