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Related Concept Videos

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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G Protein-coupled Receptors01:15

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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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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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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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An Integrated Approach for Microprotein Identification and Sequence Analysis
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An online GPCR structure analysis platform.

Albert J Kooistra1, Christian Munk2,3, Alexander S Hauser2

  • 1Department of Drug Design and Pharmacology, University of Copenhagen, Copenhagen, Denmark. albert.kooistra@sund.ku.dk.

Nature Structural & Molecular Biology
|November 11, 2021
PubMed
Summary
This summary is machine-generated.

We developed an interactive platform for comparing G-protein coupled receptor (GPCR) structures and functions. This tool aids researchers in advanced structural analysis for diverse receptor studies.

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Area of Science:

  • Biochemistry
  • Structural Biology
  • Pharmacology

Background:

  • G-protein coupled receptors (GPCRs) are crucial membrane proteins involved in numerous physiological processes.
  • Understanding GPCR structure-function relationships is vital for drug discovery and therapeutic development.
  • Existing tools often lack comprehensive comparative analysis across all available GPCR structures and functional data.

Purpose of the Study:

  • To introduce a novel online, interactive platform for the comparative analysis of all known GPCR structures.
  • To integrate structural data with functional information for a holistic understanding of GPCRs.
  • To provide researchers with a powerful tool for exploring GPCRs and designing experimental studies.

Main Methods:

  • Development of a web-based platform integrating diverse structural analysis tools.
  • Incorporation of comparative analyses including structure similarity, secondary structure, and backbone dynamics.
  • Integration of residue-residue contact networks, amino acid properties, and predictive mutagenesis design.

Main Results:

  • The platform offers a comprehensive suite of tools for in-depth GPCR structural analysis.
  • It enables direct correlation between structural features and known functional data.
  • Facilitates the identification of key structural determinants of GPCR function and potential drug targets.

Conclusions:

  • The presented platform significantly enhances the ability of researchers to analyze GPCR structures.
  • It empowers basic and applied research by providing sophisticated, integrated structural insights.
  • This resource is expected to accelerate discoveries in GPCR biology and pharmacology.