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Published on: February 20, 2018
Basic Pharmacological and Structural Evidence for Class A G-Protein-Coupled Receptor Heteromerization
Rafael Franco1, Eva Martínez-Pinilla2, José L Lanciego3
1Departament de Bioquímica i Biomedicina Molecular, Facultat de Biología, Universitat de BarcelonaBarcelona, Spain; Centro de Investigación Biomédica en Red: Enfermedades Neurodegenerativas (CIBERNED), Instituto de Salud Carlos IIIMadrid, Spain; Institute of Biomedicine, University of BarcelonaBarcelona, Spain.
Class A G-protein-coupled receptors (GPCRs) form dimers and oligomers, challenging previous assumptions. This review presents evidence for their existence in cells and natural sources, impacting pharmacology and drug discovery.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Cell membrane receptors often form complexes, but class A G-protein-coupled receptors (GPCRs) were thought to be an exception.
- Controversy exists regarding the homo- and heteromeric interactions of class A GPCRs.
Purpose of the Study:
- To review evidence supporting the existence of class A GPCR homo- and heteromers.
- To highlight the implications of class A GPCR dimerization/oligomerization for pharmacology and drug discovery.
Main Methods:
- Review of existing scientific literature and experimental data.
- Analysis of evidence from transfected cells and natural biological sources.
Main Results:
- Convergent and complementary evidence demonstrates the formation of class A GPCR homo- and heteromers.
- These interactions occur in both engineered cell systems and native biological environments.
Conclusions:
- The existence of class A GPCR homo- and heteromers is supported by substantial evidence.
- The field must now address the challenges and opportunities presented by class A GPCR dimerization for drug development and pharmacological research.
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