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Genetically-encoded Molecular Probes to Study G Protein-coupled Receptors
Published on: September 13, 2013
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GPCR-SAS: A web application for statistical analyses on G protein-coupled receptors sequences
José Carlos Gómez Tamayo1, Mireia Olivella2, Santiago Ríos1
1Laboratori de Medicina Computacional, Unitat de Bioestadística, Facultat de Medicina, Universitat Autònoma de Barcelona, Barcelona, Spain.
Plos One
|July 26, 2018
Summary
The GPCR-SAS web application offers tools for analyzing G protein-coupled receptor sequences. This aids in understanding receptor activation mechanisms and designing targeted drugs.
Area of Science:
- Biochemistry
- Structural Biology
- Pharmacology
Background:
- G protein-coupled receptors (GPCRs) are a large mammalian protein family crucial for cell signaling.
- GPCRs are significant targets for drug development due to their roles in various physiological processes.
Purpose of the Study:
- To introduce the G Protein-Coupled Receptors-Sequence Analysis and Statistics (GPCR-SAS) web application.
- To provide tools for comparative sequence analysis of GPCRs, aiding in understanding structure-function relationships.
Main Methods:
- Utilizing a curated, structure-informed multiple sequence alignment of GPCRs.
- Implementing analysis tools for amino acid/motif occurrence, entropy, covariance, and correlation at specific positions or ranges.
- Generating snake-plot representations for individual receptors or consensus sequences.
Main Results:
- Demonstrated the utility of GPCR-SAS tools for analyzing conserved residues and motifs within transmembrane segments.
- Applied the analysis to the 'transmission switch' region, critical for GPCR activation.
- Provided a freely accessible web tool for researchers.
Conclusions:
- GPCR-SAS facilitates detailed sequence analysis, offering insights into GPCR conservation and activation mechanisms.
- The tool can guide the development of more selective drug ligands.
- Comparative sequence analysis is valuable for rationalizing receptor function and drug design.
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