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A REAL-TIME ASSAY FOR Gs PROTEIN-COUPLED RECEPTORS

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
66681
Program Year/Program:
2003 / SBIR
Agency Tracking Number:
NS044641
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
ANASPEC, INC.
ANASPEC, INC. 2149 O'TOOLE AVE, STE F SAN JOSE, CA 95131
View profile »
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 2003
Title: A REAL-TIME ASSAY FOR Gs PROTEIN-COUPLED RECEPTORS
Agency: HHS
Contract: 1R43NS044641-01A1
Award Amount: $123,750.00
 

Abstract:

DESCRIPTION (provided by applicant): G protein-coupled receptors (GPCRs) are major drug targets for a wide spectrum of diseases including neurological diseases such as migraine, anxiety, psychosis, and schizophrenia Novel robust assay technologies are continuously demanded for GPCR targets to increase odds for leads generation in a large-scale compound screening. Activation of GPCRs results in changes in intracellular calcium and cAMP About 70 percent of nonchemosensory GPCRs mediate their signals through up- or down-regulation of intracellular Camp via Gs and Gi proteins respectively We propose to develop a high-throughput technology for real time assay of Gs protein-coupled receptors (Gs-GPCRs) In this application, cyclic nucleotide-gated (CNG) channel variants are specifically used as a physiological sensor for cAMP, coupling a change in intracellular cAMP concentration to changes in cytosolic calcium concentration and membrane potential Our results demonstrate that the cAMP change induced by activation of adenylyl cyclase and GPCRs can be sensitively monitored in the living mammalian cells expressing the CNG channel variants by using calcium and voltage indicators Stable cells with the sensitive CNG channel mutants have been developed to enable the assay in 96-well microplates This convenient assay allows for the kinetic detection of transient cAMP signals with a high signal-tonoise ratio CNG channels may also provide a means to detect local cAMP concentrations in proximity to adenylylcyclase, allowing for a sensitive detection of GPCR activity Towards next stage of commercialization, we propose to further improve and adapt this robust GPCR assay to standard high-throughput screening platforms including FLIPR.

Principal Investigator:

Yong Yao
3013407320
yyao@atto.com

Business Contact:


2406834500
Small Business Information at Submission:

APTUS PHARMACEUTICALS, INC.
APTUS PHARMACEUTICALS, INC. 101 ORCHARD RIDGE DR, 1E GAITHERSBURG, MD 20878

EIN/Tax ID: 522248374
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No