Award
National Institute of General Medical Sciences 5R01GM124093-08
PHARMACOLOGICAL TARGETING OF GALPHA SUBUNITS IN DISEASE
Recipient
Washington University, Saint Louis, MO
Award Amount
$460,566.00
Ceiling
$460,566.00
Awarded
July 15, 2024
Identifier
5R01GM124093-08
NIH funded project to develop bioavailable inhibitors targeting G protein α-subunits for diseases including cancers and Alzheimer's, using advanced chemical and biological techniques.
Description
This multi-PI basic science project aims to understand G-protein function in physiology and disease, and develop therapeutics for untreatable diseases caused by mutant G protein α-subunits. It involves designing and synthesizing bioavailable inhibitors that selectively target groups of heterotrimeric G proteins, with potential applications in diseases such as uveal melanoma, pituitary tumors, mucosal melanoma, and others. The project will address challenges related to inhibitor availability, targeting, mechanism understanding, and subtype selectivity, using synthetic organic chemistry, computational docking, single-molecule FRET, NMR, and biochemical assays.