# Structure and dynamics of G protein coupled receptor-G protein complexes

> **NIH NIH R01** · UNIVERSITY OF CALIFORNIA, SAN DIEGO · 2023 · $69,045

## Abstract

Project Summary
G protein-coupled receptors (GPCRs) are important conduits to relay extracellular
signals to downstream intracellular signal transduction pathways. In addition to being a
central mode of intercellular communication the magnitude of the gene family and their
structural diversity make GPCRs superb targets for therapeutics. Understanding the
mechanism of hormone action on GPCRs and understanding how drugs modulate their
behavior is an important fundamental endeavor but also an important mission for health
scientists. The primary goal of this proposal is to study the mechanism of GPCR
regulation of their primary signaling partners, G proteins. We will take a biochemical
and biophysical approach to understand the mechanism of GPCR·G protein interactions
and determine how agonist activation of GPCRs leads to G protein activation. We will
utilize cutting-edge approaches including x-ray crystallography, cryo-electron
microscopy, double electron-electron resonance spectroscopy and single molecule
spectroscopy to study these receptor-G protein interactions. A critical component of
these studies is obtaining sufficient quantities of purified preparations of G protein-
coupled receptors and heterotrimeric G proteins, as well as other critical reagents such
as nanobodies. In our studies, the use of chromatography and in particular, fast
performance liquid chromatography (FPLC) is an essential approach to obtaining our
purified preparations. This is an ongoing research grant, now in its 16th year and our
instrumentation for liquid chromatography is becoming obsolete. In my laboratory more
and more trainees requiring the use of our current FPLC instrumentation, which are now
between 20 and 25 years old. The instruments have been experiencing significant
downtime, requiring more and more costly service and repair. More importantly, parts
are now starting to be no longer available. We propose to update our instrumentation
for this critical component of our research on the biochemistry, biophysics and structural
pharmacology of interaction between G protein and GPCRs.

## Key facts

- **NIH application ID:** 10799459
- **Project number:** 3R01GM083118-16S1
- **Recipient organization:** UNIVERSITY OF CALIFORNIA, SAN DIEGO
- **Principal Investigator:** Brian K Kobilka
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2023
- **Award amount:** $69,045
- **Award type:** 3
- **Project period:** 2008-05-01 → 2025-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10799459

## Citation

> US National Institutes of Health, RePORTER application 10799459, Structure and dynamics of G protein coupled receptor-G protein complexes (3R01GM083118-16S1). Retrieved via AI Analytics 2026-05-25 from https://api.ai-analytics.org/grant/nih/10799459. Licensed CC0.

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