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Related Concept Videos

GPCRs Regulate Adenylyl Cylase Activity01:09

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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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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.
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Transducer Mechanism: G Protein–Coupled Receptors01:30

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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.
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Pulmonary Hypertension: Classification and Pathogenesis01:30

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Pulmonary hypertension (PH) is a severe health condition in which the mean pulmonary arterial pressure increases to 25 mmHg or more, even when the body is at rest. This high pressure in the blood vessels that transport blood from the heart to the lungs can cause various symptoms, including shortness of breath, can lead to right heart failure, and significantly affect the overall quality of life.
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G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
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Adhesion GPCR Function in Pulmonary Development and Disease.

Marie-Gabrielle Ludwig1, Klaus Seuwen1, James P Bridges2,3

  • 1Novartis Institutes for Biomedical Research, Basel, 4056, Switzerland.

Handbook of Experimental Pharmacology
|November 11, 2016
PubMed
Summary
This summary is machine-generated.

Adhesion GPCRs (aGPCRs) are increasingly recognized for their roles in lung development and disease. This review focuses on available data for aGPCRs in pulmonary biology, highlighting Adgrf5.

Keywords:
Alveolar epitheliumCOPDLung developmentLung diseaseLung homeostasisPulmonary surfactant

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Area of Science:

  • Pulmonary Biology
  • Cellular Signaling
  • Molecular Medicine

Background:

  • G-protein-coupled receptors (GPCRs) are crucial in pulmonary physiology and disease treatment.
  • Adhesion GPCRs (aGPCRs) are an emerging class with significant, yet understudied, roles in lung biology.
  • Current understanding of aGPCRs in pulmonary contexts is limited but growing.

Purpose of the Study:

  • To review existing literature on adhesion GPCRs (aGPCRs) in pulmonary biology.
  • To highlight the known functions and implications of aGPCRs in lung development, homeostasis, and disease.
  • To focus on Adgrf5, the aGPCR with the most available data in this field.

Main Methods:

  • Literature review of studies involving aGPCRs and pulmonary systems.
  • Analysis of data from loss-of-function experiments and pharmacologic studies.
  • Synthesis of current knowledge regarding specific aGPCRs, particularly Adgrf5.

Main Results:

  • Classic GPCRs extensively influence lung function and are therapeutic targets.
  • Adhesion GPCRs (aGPCRs) play critical roles in lung development, maintenance, and pathology.
  • Adgrf5 is the most studied aGPCR in the pulmonary system to date, with substantial data emerging.

Conclusions:

  • Adhesion GPCRs (aGPCRs) represent a promising area for understanding and treating pulmonary diseases.
  • Further research into aGPCRs, especially Adgrf5, is warranted to elucidate their full therapeutic potential.
  • This review consolidates current knowledge, serving as a foundation for future investigations into aGPCRs in lung biology.