# Next generation GPCR drug discovery

> **NIH NIH R43** · SEVEN BIOSCIENCES, INC. · 2020 · $221,400

## Abstract

PROJECT SUMMARY/ ABSTRACT
Drugs targeting G-protein coupled receptors (GPCRs) represent 25% of the 100 top grossing drugs and make
up 35% of all Food and Drug Administration (FDA) approved drugs. GPCRs are integral membrane receptors
which transduce extracellular signals into a variety of intracellular responses. GPCRs represent the largest family
of druggable targets due to their expression in nearly every organ system, accessibility on the membrane and
potential to elicit almost every signaling pathway. Despite relative success in pharmacologically targeting GPCRs
for treating neurological and psychiatric disorders such as Parkinson’s disease, schizophrenia, depression and
addiction, the identification of novel neural drugs with alleviated side-effects is still a formidable challenge largely
due to limited technology. Therefore, it is critical to develop technology that will enable the discovery of novel
compounds with minimal side-effects such as fast-acting and long-lasting nonaddictive and nonhallucinogenic
antidepressant drugs. Numerous studies have shown that ligands stabilize distinct structural conformations of
single receptors with varying efficacies which can lead to the activation of a signaling pattern of therapeutic
advantage. Though these modulators have been suggested to be the key to therapeutic advancement, the path
to discovery has been hindered by the lack of technology that permits quantitative analysis of the diverse
functional conformation dynamics of GPCRs on a large-scale. Therefore, we propose to further validate and
apply our patented platform technology based on GPCR conformer sensors which enables imaging of real-time
pharmacodynamics to identify functionally selective GPCR targets in high-throughput.

## Key facts

- **NIH application ID:** 10082377
- **Project number:** 1R43MH122078-01A1
- **Recipient organization:** SEVEN BIOSCIENCES, INC.
- **Principal Investigator:** Grace Mizuno
- **Activity code:** R43 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $221,400
- **Award type:** 1
- **Project period:** 2020-07-01 → 2021-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10082377

## Citation

> US National Institutes of Health, RePORTER application 10082377, Next generation GPCR drug discovery (1R43MH122078-01A1). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/10082377. Licensed CC0.

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