Abstract

Abstract The small GTPase KRAS is a known oncogene that is very frequently mutated in a variety of cancers. Over the past several years, there has been a resurgence of interest in KRAS drug discovery following the identification of new inhibitor target sites and several molecules entering clinical trials. We have produced proteins and set up assays for a large collection of Ras variants, guanine nucleotide exchange factors and effectors to facilitate drug discovery activities targeting KRAS/MAPK pathway. RBC’s extensive kinase assay portfolio enables identification of kinase inhibitors downstream of Ras. This poster will summarize our most recent assay development efforts for biochemical and biophysical assays for these targets. Citation Format: Ekaterina Kouznetsova, Lauren S. McCauley, Rebecca Eells, Elaine Steinke-Neal, Timothy Sullivan, Louis Primavera, Charles Longen, Haiching Ma. Assay toolkit for the discovery of new RAS pathway inhibitors [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2023; Part 1 (Regular and Invited Abstracts); 2023 Apr 14-19; Orlando, FL. Philadelphia (PA): AACR; Cancer Res 2023;83(7_Suppl):Abstract nr 2624.

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