Illuminating the Druggable GPCR-ome

NIH RePORTER · NIH · U24 · $749,510 · view on reporter.nih.gov ↗

Abstract

Abstract PROJECT SUMMARY G protein coupled receptors (GPCRs) represent essential molecular targets for a large number of approved as well as investigational medications. Of the 380 or so non-olfactory GPCRs in the human genome around 100 are understudied and/or orphan receptors (oGPCRs). The oGPCRs represent potential therapeutic targets although discovering drugs that modulate them is challenging. Here we will solve the structures of 15-20 oGPCRs using cryogenic electron microscopy (cryo-EM). The solved structures then will serve as templates for structure-guided drug discovery targeting these oGPCRs.

Key facts

NIH application ID
10612133
Project number
3U24DK116195-05S1
Recipient
UNIV OF NORTH CAROLINA CHAPEL HILL
Principal Investigator
Bryan L. Roth
Activity code
U24
Funding institute
NIH
Fiscal year
2022
Award amount
$749,510
Award type
3
Project period
2017-09-15 → 2023-08-31