# Functional Genomics of G Protein-Coupled Receptors

> **NIH NIH R43** · OCTANT, INC. · 2020 · $246,943

## Abstract

G protein-coupled receptors (GPCRs) are central mediators of mammalian cells’ ability to sense and respond
to their environment. The 813 human GPCRs are the largest class of membrane receptors, are central
mediators of cell physiology, and are the target of ~34% of all U.S. Food and Drug Administration
(FDA)-approved drugs and ~60% of prescriptions. Here we will leverage recent advances in DNA synthesis,
genome editing, next-generation DNA sequencing, and informatics develop a platform to build thousands of
individual mutations to GPCRs and experimentally characterize their effects in a novel assay that can be done
in a simple pooled format in human cell lines. We will develop methodologies to characterize how these
mutational libraries functionally signal through the two major pathways that GPCRs signal through, the cyclic
AMP and calcium signaling pathways. The profiles will give us the ability to better understand the functional
consequences of genetic variation in GPCRs and how they might be impacting diseases and drug responses.
In addition, analysis of these mutational profiles will give us insights on how to target these receptors for
making new drugs. The technologies developed here should be broadly and directly applicable to the vast
majority of GPCRs, as well as other important classes of drug targets where function can be assessed by
transcriptional reporters in human cell lines.

## Key facts

- **NIH application ID:** 10010909
- **Project number:** 1R43GM137745-01
- **Recipient organization:** OCTANT, INC.
- **Principal Investigator:** Sriram Kosuri
- **Activity code:** R43 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $246,943
- **Award type:** 1
- **Project period:** 2020-05-01 → 2020-10-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10010909

## Citation

> US National Institutes of Health, RePORTER application 10010909, Functional Genomics of G Protein-Coupled Receptors (1R43GM137745-01). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10010909. Licensed CC0.

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