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Related Concept Videos

G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

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GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory...
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GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

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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...
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cAMP-dependent Protein Kinase Pathways01:25

cAMP-dependent Protein Kinase Pathways

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Cyclic Adenosine Monophosphate (cAMP) is an essential second messenger that activates protein kinase A (PKA) and regulates various biological processes. A single epinephrine molecule binds to GPCR and activates several heterotrimeric G proteins, each stimulating multiple adenylyl cyclase, amplifying the signal, and synthesizing large numbers of cAMP molecules. Small changes in cAMP concentration affect PKA activity. The binding of four cAMP molecules induces a conformational change in PKA,...
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Blood Studies for Cardiovascular System II: CRP, Hcy, and Cardiac Natriuretic Peptide Markers01:19

Blood Studies for Cardiovascular System II: CRP, Hcy, and Cardiac Natriuretic Peptide Markers

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Cardiac biomarkers are critical in diagnosing, prognosing, and managing cardiovascular diseases. Routine measurement of specific biomarkers such as B-type natriuretic peptide (BNP), C-reactive protein (CRP), and homocysteine (Hcy) is common practice in clinical settings to evaluate heart function and predict cardiovascular events.
These markers indicate stress or strain on the heart muscle:
Natriuretic Peptides (BNP)
Cardiac myocytes produce these hormones in response to ventricular stretching...
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GPCR Desensitization01:12

GPCR Desensitization

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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...
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G-protein Coupled Receptors01:21

G-protein Coupled Receptors

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Related Experiment Video

Updated: Apr 12, 2026

In vitro Assessment of Cardiac Reprogramming by Measuring Cardiac Specific Calcium Flux with a GCaMP3 Reporter
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GPCR signaling and cardiac function.

Leany A Capote1, Roberto Mendez Perez1, Anastasios Lymperopoulos1

  • 1From the Laboratory for the Study of Neurohormonal Control of the Circulation, Department of Pharmaceutical Sciences, Nova Southeastern University College of Pharmacy, Fort Lauderdale, FL 33328, USA.

European Journal of Pharmacology
|May 19, 2015
PubMed
Summary
This summary is machine-generated.

G protein-coupled receptors (GPCRs) are vital for heart function and are targeted by many cardiovascular drugs. Research is identifying new GPCR-related targets for future heart disease therapies.

Keywords:
CardiacContractilityG protein-coupled receptorSignalingTherapeutic target

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Area of Science:

  • Cardiology
  • Molecular Biology
  • Pharmacology

Background:

  • G protein-coupled receptors (GPCRs) are crucial for cardiac function and morphology.
  • They are targets for over a third of approved cardiovascular drugs.
  • GPCRs are present in myocytes, fibroblasts, and endothelial cells.

Purpose of the Study:

  • To review GPCR signaling pathways in cardiac myocytes.
  • To highlight current drugs targeting cardiac GPCRs.
  • To identify potential novel drug targets in cardiac GPCR signaling.

Main Methods:

  • Review of scientific literature on GPCRs in the heart.
  • Analysis of signaling pathways modulated by GPCRs.
  • Identification of existing and potential drug targets.

Main Results:

  • GPCRs directly modulate cardiac contractility.
  • Numerous drugs target cardiac GPCRs for cardiovascular conditions.
  • Emerging molecular targets within GPCR signaling pathways exist.

Conclusions:

  • GPCRs are essential regulators of cardiac function and disease.
  • Current therapies leverage GPCRs, with ongoing discovery of new targets.
  • Targeting cardiac GPCR signaling offers future therapeutic potential for heart disease.