Project 171171

Molecular basis of GPCR internalization and trafficking

171171

Molecular basis of GPCR internalization and trafficking

$666,970
Project Information
Study Type: Other Mechanistic_Study
Therapeutic Area: Cardiovascular
Research Theme: Biomedical
Disease Area: hypertension, inflammation, pain
Data Type: Canadian
Institution & Funding
Principal Investigator(s): Laporte, Stéphane A
Institution: McGill University Health Centre
CIHR Institute: Circulatory and Respiratory Health
Program: Operating Grant
Peer Review Committee: Pharmacology & Toxicology
Competition Year: 2008
Term: 5 yrs 0 mth
Abstract Summary

G protein coupled receptors (GPCRs) are the single largest family of cell surface proteins involved in signal transduction, and represent one of the major pharmaceutical targets. Action of drugs and hormones are intricately linked to the constant presence of these receptors on the cells surface, which in normal condition is regulated by the internalization and intracellular trafficking processes. Deregulation of these processes can lead to abnormal cell behaviors, and the development of pathological conditions. Although we have gain a basic understanding of some of the components for receptor internalization and trafficking, much remains to be understood on the signaling mechanisms and regulators involved in these events. Her we propose to use innovative molecular and cell biological approaches to identify and study key regulators for the internalization and intracellular trafficking of the angiotensin and bradykinin receptors; two GPCRs that are important drug targets in cardiovascular therapies. We believe that our study will not only provide new insights into the molecular details for these events, but may also help identifying new targets to improve drug efficiency for hypertension, inflammation and pain.

Research Characteristics

This project includes the following research characteristics:

Knowledge Translation Focus
Biomarker Endpoints
Study Justification

"Her we propose to use innovative molecular and cell biological approaches to identify and study key regulators for the internalization and intracellular trafficking of the angiotensin and bradykinin receptors; two GPCRs that are important drug targets in cardiovascular therapies."

Novelty Statement

"We believe that our study will not only provide new insights into the molecular details for these events, but may also help identifying new targets to improve drug efficiency for hypertension, inflammation and pain."

Methodology Innovation

using innovative molecular and cell biological approaches to study the internalization and intracellular trafficking of GPCRs, which may identify new drug targets

Keywords
Arrestins Biochemistry Cell Biology Clathrin-Mediated Internalization Confocal Microscopy Congestive Heart Failure