# A New Versatile, SERS-based GPCR assay

> **NIH NIH R43** · VICOLINE MEDICAL, LLC · 2021 · $259,613

## Abstract

PROJECT SUMMARY
G protein-coupled receptors (GPCRs) represent one of the highest priority targets for the pharmaceutical industry
and roughly one-third of all approved drugs target on specific GPCRs, which corresponds to global sales of over
USD 180 billion annually. As one of the largest gene families in humans with varied physiology functions, GPCRs
have also been implicated in the pathophysiology of numerous diseases such as cancer, diabetes insipidus,
heart disease, and numerous metabolic disorders. Understanding the characteristics of GPCRs remains a
central theme in biology and various commercial assays are available to characterize ligand binding affinity and
the identification of agonists and antagonists for members of this receptor family. Despite their utility, these
assays have a number of limitations that preclude their widespread use. These include the need for expensive,
artificial GPCR cell lines; limited analytical output; indirect measures of GPCR properties; and the potential for
photobleaching and photodamage during data collection. Surface-enhanced Raman spectroscopy (SERS) is an
extremely sensitive and highly specific means to analyze surface molecules in the cellular and subcellular
domains. The proposed Phase I research plan focuses on the development of SERS-based probes for the
characterization of two GPCRs that are members of the predominant class of these receptors, the Class A GPCR
family. This approach has noted advantages over existing technology including greater analytical output, direct
measures of the GPCR rather than downstream targets, and the ability to apply this technology to any native
cells with their normal complement of cellular proteins. The long-term goal of this research is to develop a low
cost, versatile and robust platform for the characterization of GPCRs that is a significant advancement over those
assays currently available. To meet this goal, we have the following specific objectives.
• Development of GPCR SERS probes (Specific Aim 1). The initial goal (Obj. 1.1) in this part of the proposed
plan is to identify suitable antibodies for eventual construction of SERS probes using immunohistochemistry and
surface plasma resonance for GPR84 and GPR120 in cell lines expressing these receptors. Objective 1.2 will
use the identified antibodies to synthesize, construct and characterize SERS probes specific for GPR84 and
GPR120.
• Development of the SERS-based GPCR activation assay and validation with existing technology
(Specific Aim 2). The SERS probes will be used in Objective 2.1 to develop the point-by-point and spectral
mapping modules to provide the kinetic analyses, dose-dependence, relative expression area, and activation
probabilities for these two GPCRs. Data generated in this objective will be compared to the exiting technology
by running commercially available assays (PathHunter® ß-arrestin assays; Eurofins) on the same two cell lines
(Objective 2.2).

## Key facts

- **NIH application ID:** 10324451
- **Project number:** 1R43GM144020-01
- **Recipient organization:** VICOLINE MEDICAL, LLC
- **Principal Investigator:** Wei Zhang
- **Activity code:** R43 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $259,613
- **Award type:** 1
- **Project period:** 2021-09-01 → 2023-08-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10324451

## Citation

> US National Institutes of Health, RePORTER application 10324451, A New Versatile, SERS-based GPCR assay (1R43GM144020-01). Retrieved via AI Analytics 2026-05-26 from https://api.ai-analytics.org/grant/nih/10324451. Licensed CC0.

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