Developing a Chemically-Controlled RAS Toolset

NIH RePORTER · NIH · F31 · $44,695 · view on reporter.nih.gov ↗

Abstract

Project Abstract RAS GTPase operates as a molecular switch toggling between GDP-bound (inactive) and GTP-bound forms (active), and orchestrates dynamic cellular processes such as proliferation, migration, survival, and T-cell development.1,2 Despite its binary nature, RAS exhibits sophisticated and dynamic signaling behavior influenced by cellular context and subcellular localization. The lack of a precise understanding of the roles of spatiotemporal compartmentalization in RAS hinders our understanding of fundamental signaling mechanisms and limits our ability to develop targeted therapies for RAS-driven cancers. To address this, we will leverage a chemical genetic tool called Chemically-Inducible Activator of RAS (CIAR) that allows the rapid and dose-dependent activation of wild-type RAS with bio-orthogonal small molecules.8-10 Aim 1 describes efforts to use transmembrane-tethered versions of NS3a-CIAR to dissect the impact of differential membrane localization on wild-type RAS activation and downstream signaling. This Aim also describes the development of chemical tools for quantitatively measuring the transmembrane localization of proteins and using a novel tool for probing RAS-GTP in its native cellular context. Aim 2 aims to investigate the role of oligomerization of signaling proteins at membranes. An engineered protein toolkit will be used to control the oligomeric state and study its impact on Ras-mediated signaling. Finally, Aim 3 explores efforts to dissect how the intracellular signaling environment affects the kinetics of magnitude of RAS activation and downstream signaling. This Aim also explores the development of a number of chemical genetic tools for enabling intracellular protein display at membranes. Overall, the studies described herein will offer new and important mechanistic insight into RAS signaling.

Key facts

NIH application ID
10995224
Project number
1F31GM155953-01
Recipient
UNIVERSITY OF WASHINGTON
Principal Investigator
Fernando Banales Mejia
Activity code
F31
Funding institute
NIH
Fiscal year
2024
Award amount
$44,695
Award type
1
Project period
2024-09-01 → 2027-08-31