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Updated: Aug 9, 2025

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
Published on: June 9, 2017
Advances in the molecular level understanding of G-protein coupled receptor
1Amity Institute of Molecular Medicine & Stem Cell Research, Amity University, Noida, Uttar Pradesh, India.
Abstract:
G-protein coupled receptors (GPCRs) represent largest family of plasma membrane-bound receptor proteins that are involved in numerous cellular and physiological functions. Many extracellular stimuli such as hormones, lipids and chemokines activate these receptors. Aberrant expression and genetic alteration in GPCR are associated with many human diseases including cancer and cardiovascular disease. GPCRs have emerged as potential therapeutic target and numerous drugs are either approved by FDA or under clinical trial. This chapter provides an update on GPCR research and its significance as a promising therapeutic target.
Insights
G-protein coupled receptors (GPCRs) are key cell signaling proteins. Research highlights their role in diseases and their potential as drug targets, with many therapies in development.
Area of Science:
- Biochemistry and Molecular Biology
- Cellular Signaling
- Pharmacology
Background:
- G-protein coupled receptors (GPCRs) are the largest family of cell surface receptors.
- They mediate cellular responses to diverse extracellular signals like hormones and chemokines.
- Dysregulation of GPCRs is implicated in major human diseases.
Purpose of the Study:
- To provide an updated overview of G-protein coupled receptor (GPCR) research.
- To emphasize the significance of GPCRs as therapeutic targets.
- To highlight current drug development efforts targeting GPCRs.
Main Methods:
- Literature review of current GPCR research.
- Analysis of GPCR involvement in human diseases.
- Survey of approved and investigational drugs targeting GPCRs.
Main Results:
- GPCRs play critical roles in numerous cellular and physiological processes.
- Aberrant GPCR expression and genetic mutations are linked to cancer and cardiovascular diseases.
- A significant number of GPCR-targeting drugs are available or in clinical trials.
Conclusions:
- G-protein coupled receptors (GPCRs) are vital for cell communication and function.
- GPCRs represent a highly promising area for therapeutic intervention.
- Continued research into GPCRs is essential for developing novel treatments for various diseases.
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