Abstract
Abstract The small GTPase, KRAS, is a known oncogene and a desirable drug target due to prevalence of mutations with poor disease prognosis. The absence of good druggable binding pockets has made modulator compound discovery challenging and unsuccessful. Identification of new inhibitor target sites has led to the resurgence of interest in KRAS drug discovery. To facilitate drug discovery activities targeting KRAS/MAPK pathway, we have produced the full spectrum of pathway proteins including kinases, wild type and mutated KRAS, guanine nucleotide exchange factor and effectors. This poster will summarize our most recent assay development efforts for biochemical and biophysical assays for these targets. Citation Format: Ekaterina Kouznetsova, Lauren McCauley, Elaine Steinke-Neal, Timothy Sullivan, Louis Primavera, Rebecca Eells, Haiching Ma. A versatile assay suite for the discovery of new KRAS pathway inhibitors [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2022; 2022 Apr 8-13. Philadelphia (PA): AACR; Cancer Res 2022;82(12_Suppl):Abstract nr 2987.
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