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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

G Protein Coupled Receptors And Structure-Based Advances

Author(s): Maria Kontoyianni

Volume 16 , Issue 13 , 2016

Page: [1489 - 1505] Pages: 17

DOI: 10.2174/1568026615666150915121324

Price: $65

Abstract

G protein coupled receptors (GPCRs) are membrane proteins coupled with G proteins through which they transmit signals to the cytoplasm. Approximately 30% of pharmaceuticals target these receptors, even though crystal structures were scarce at the time. Furthermore, an additional 15% of GPCRs have yet to be exploited for therapeutic intervention. An overview of structural information is presented, with emphasis on rearrangements occurring during activation,in light of recently resolved activated state crystal structures. Computational efforts over recent years are also highlighted.

Keywords: G Protein Coupled Receptors, Homology Modeling, Virtual Screening, Model-Building, Critical Assessment of Structure Prediction, Docking, Structure-Based Drug Design, Activation Mechanisms, Conserved Motifs.

Graphical Abstract

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