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PCR

PCR

GPCRs Regulate Adenylyl Cylase Activity

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...

GPCR Desensitization

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...

PCR - Polymerase Chain Reaction

PCR - Polymerase Chain Reaction

CRISPR

CRISPR

Genome editing technologies allow scientists to modify an organism’s DNA via the addition, removal, or rearrangement of genetic material at specific genomic locations. These types of techniques could potentially be used to cure genetic disorders such as hemophilia and sickle cell anemia. One popular and widely used DNA-editing research tool that could lead to safe and effective cures for genetic disorders is the CRISPR-Cas9 system. CRISPR-Cas9 stands for Clustered Regularly Interspaced Short...

G Protein-coupled Receptors

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...

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Related Experiment Video

Updated: Jun 20, 2026

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

Published on: April 9, 2018

GPCR theme editorial.

G Milligan, J C McGrath

British Journal of Pharmacology

|September 2, 2009

Summary

This summary is machine-generated.

G-protein coupled receptors (GPCRs) are crucial drug targets. This collection explores their biology, pharmacology, and diverse therapeutic applications, from pain to cancer.

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Last Updated: Jun 20, 2026

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

Optimizing the Genetic Incorporation of Chemical Probes into GPCRs for Photo-crosslinking Mapping and Bioorthogonal Chemistry in Live Mammalian Cells

Published on: April 9, 2018

Development of a Quantitative Recombinase Polymerase Amplification Assay with an Internal Positive Control

Development of a Quantitative Recombinase Polymerase Amplification Assay with an Internal Positive Control

Published on: March 30, 2015

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery

Published on: June 28, 2019

Area of Science:

Pharmacology
Molecular Biology
Drug Discovery

Background:

G-protein coupled receptors (GPCRs) represent a major class of cell surface receptors and a significant focus for drug development.
This themed collection covers recent advances in GPCR biology and pharmacology, encompassing molecular interactions and signaling pathways.

Discussion:

Explores receptor hetero-dimerization, interactions with signaling molecules like cAMP and G12/13 proteins, and novel de-orphanised receptors (Neuromedins U & S, FFA2 & FFA3).
Reviews the pharmacology of diverse GPCRs, including adrenoceptors, purinoceptors, 5HT, opioid, cannabinoid, and PAR-2 receptors.
Highlights the expanding role of GPCRs in physiological systems and therapeutic areas such as pain, cancer, cardiovascular, gastrointestinal, visual, respiratory, and central nervous systems.

Key Insights:

Focus on the rapidly developing pharmacology of drugs targeting beta(2)-adrenoceptors.
Emphasizes the broad therapeutic potential of targeting GPCRs across multiple disease states.
Advances understanding of GPCR molecular mechanisms and drug interactions.

Outlook:

GPCRs continue to be central to understanding and treating a wide array of human diseases.
Future research will likely focus on novel GPCR targets and sophisticated drug development strategies.
The insights presented will guide future therapeutic interventions targeting GPCRs.