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Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists01:23

Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists

Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors01:20

Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors

Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
G Protein-coupled Receptors01:15

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...
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical, 7TM, or...
Integrins01:10

Integrins

Animal and protozoan cells do not have cell walls to help maintain shape and provide structural stability. Instead, these eukaryotic cells secrete a sticky mass of carbohydrates and proteins into the spaces between adjacent cells. This network of proteins and molecules is called an extracellular matrix or ECM.
Some ECM proteins assemble into a basement membrane to which the remaining components adhere. Proteoglycans typically form the bulk of the ECM while fibrous proteins, like collagen,...

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Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
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The human prostacyclin receptor from structure function to disease.

Kathleen A Martin1, Scott Gleim, Larkin Elderon

  • 1Department of Pharmacology and Toxicology, Dartmouth Medical School, Hanover, New Hampshire 03755, USA.

Progress in Molecular Biology and Translational Science
|April 9, 2010
PubMed
Summary

Prostacyclin, a substance that relaxes arteries, plays a key role in conditions like atherothrombosis, pain, and inflammation. Research into prostacyclin receptor function and signaling pathways is paving the way for new therapies.

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Last Updated: Jun 14, 2026

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Area of Science:

  • Cardiovascular Biology
  • Pharmacology
  • Molecular Medicine

Background:

  • Prostacyclin (prostanoid X) was first identified 30 years ago for its vasodilatory effects on mesenteric arteries.
  • Recent studies highlight prostacyclin's critical role in atherothrombosis, pain, inflammation, and parturition.
  • Dysfunctional prostacyclin receptor genetic variants and selective cyclooxygenase-2 inhibition clinical trials underscore its pathophysiological significance.

Purpose of the Study:

  • To review the evolving understanding of prostacyclin's role in health and disease.
  • To explore the potential of prostacyclin-based therapies beyond pulmonary hypertension.
  • To emphasize the importance of structure-function studies for the prostacyclin receptor and its signaling pathways.

Main Methods:

  • Review of recent research including receptor knockout mice studies.
  • Analysis of clinical trial data from selective cyclooxygenase-2 inhibition.
  • Examination of genetic variant studies related to prostacyclin receptors.

Main Results:

  • Prostacyclin is implicated in diverse pathophysiological conditions, including atherothrombosis, pain, and inflammation.
  • Prostacyclin receptor genetic variants can be dysfunctional, impacting its signaling.
  • Emerging evidence supports prostacyclin-based therapies for a broader range of diseases.

Conclusions:

  • Prostacyclin's significance in various physiological and pathological processes is increasingly recognized.
  • Further research into prostacyclin receptor structure and signal transduction is crucial.
  • Prostacyclin-based therapies hold promise for treating conditions beyond pulmonary hypertension.