WebThese findings suggest that pan-RAS inhibition may be an effective therapeutic strategy for some cancers and that structure-based design of small molecules targeting multiple adjacent sites to create multivalent inhibitors may be effective for some proteins. Google Scholar PubMed Columbia University Cornell University Genentech WebTargeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor Highlights • ARS-1620, an atropisomeric selective KRAS G12C inhibitor with desirable PK • ARS-1620 selectively induces tumor regression in patient-derived tumor models • KRAS dependency is more profound in vivo compared to 2D-monolayer cell culture •
Multivalent Small-Molecule Pan-RAS Inhibitors - PubMed
Web23 feb. 2024 · Design of small molecules that disrupt protein-protein interactions, including the interaction of RAS proteins and their effectors, have potential use as chemical probes and therapeutic agents. We describe here the synthesis and testing of potential small molecule pan-RAS ligands, which were designed to interact with adjacent sites on the … WebThese findings suggest that pan-RAS inhibition may be an effective therapeutic strategy for some cancers and that structure-based design of small molecules targeting multiple … healthcare it jobs california
Multivalent small molecule pan-RAS inhibitors – ScienceOpen
WebMultivalent Small-Molecule Pan-RAS Inhibitors. by Matthew E Welsch, Anna Kaplan, Jennifer M Chambers, Michael E Stokes, Pieter H Bos, Arie Zask, Yan Zhang, Marta Sanchez-Martin, Michael A Badgley, Christine S Huang, Timothy H Tran, Hemanth Akkiraju, Lewis M Brown, Renu Nandakumar, Serge Cremers, Wan Seok Yang, Liang Tong, … Web31 ian. 2024 · RAS proteins were among the first oncoproteins to be targeted with small molecules, albeit indirectly. At a time when kinases were viewed with suspicion, the opportunity to inactivate RAS proteins by inhibiting enzymes, their prenylation seemed feasible and attractive, and, with this goal in mind, farnesyl transferase inhibitors with … Web23 feb. 2024 · These findings suggest that pan-RAS inhibition may be an effective therapeutic strategy for some cancers, and that structure-based design of small … healthcare it jobs atlanta