Ontology highlight
ABSTRACT:
SUBMITTER: Welsch ME
PROVIDER: S-EPMC5362268 | biostudies-literature | 2017 Feb
REPOSITORIES: biostudies-literature
Welsch Matthew E ME Kaplan Anna A Chambers Jennifer M JM Stokes Michael E ME Bos Pieter H PH Zask Arie A Zhang Yan Y Sanchez-Martin Marta M Badgley Michael A MA Huang Christine S CS Tran Timothy H TH Akkiraju Hemanth H Brown Lewis M LM Nandakumar Renu R Cremers Serge S Yang Wan Seok WS Tong Liang L Olive Kenneth P KP Ferrando Adolfo A Stockwell Brent R BR
Cell 20170201 5
Design of small molecules that disrupt protein-protein interactions, including the interaction of RAS proteins and their effectors, may provide 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 surface of oncogenic KRAS. One compound, termed 3144, was found to bind to RAS proteins using microscale thermophoresis, nuclear magnetic resonance spectroscopy, and iso ...[more]