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Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
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G protein-coupled receptors: the evolution of structural insight
Samantha B Gacasan1, Daniel L Baker1, Abby L Parrill1
1Department of Chemistry, University of Memphis, 3744 Walker Ave, Memphis, TN 38152, USA.
AIMS Biophysics
|June 29, 2018
Summary
G protein-coupled receptors (GPCRs) are key drug targets. Recent technological advances have enabled the determination of over 180 GPCR structures, revealing diverse functional states.
Area of Science:
- Biochemistry
- Structural Biology
- Pharmacology
Background:
- G protein-coupled receptors (GPCRs) are a large protein superfamily crucial for cellular signaling.
- GPCRs represent significant targets for pharmaceutical drug development.
- High-resolution three-dimensional structures of GPCRs have only recently become accessible.
Purpose of the Study:
- To review technological advancements enabling GPCR structural determination.
- To present a comprehensive list and comparative analysis of known GPCR structures.
- To summarize GPCR functional states captured in various crystalline forms.
Main Methods:
- Review of published literature on GPCR structure determination.
- Analysis of crystallographic data for over 180 GPCR structures.
- Categorization of structures based on bound ligands and functional states.
Main Results:
- Technological progress, starting with rhodopsin (PDB: 1F88) in 2000, has led to over 40 unique GPCR structures.
- A comprehensive catalog of over 180 GPCR structures is presented.
- Structures represent diverse GPCRs crystallized with agonists, antagonists, and allosteric modulators.
Conclusions:
- Recent structural biology breakthroughs have significantly advanced GPCR research.
- The availability of numerous GPCR structures facilitates drug discovery and design.
- Understanding GPCR structural diversity and functional states is critical for therapeutic development.
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