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Current Trends in GPCR Allostery.

Authors
  • Singh, Khuraijam Dhanachandra1
  • Karnik, Sadashiva S2
  • 1 Department of Cardiovascular and Metabolic Sciences, Cleveland Clinic Lerner College of Medicine at Case Western Reserve University, Cleveland Clinic, 9500 Euclid Avenue, Cleveland, OH, 44195, USA.
  • 2 Department of Cardiovascular and Metabolic Sciences, Cleveland Clinic Lerner College of Medicine at Case Western Reserve University, Cleveland Clinic, 9500 Euclid Avenue, Cleveland, OH, 44195, USA. [email protected]
Type
Published Article
Journal
The Journal of Membrane Biology
Publisher
Springer-Verlag
Publication Date
Jun 01, 2021
Volume
254
Issue
3
Pages
293–300
Identifiers
DOI: 10.1007/s00232-020-00167-6
PMID: 33471142
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

GPCRs remain the most important drug target comprising ~ 34% of the Food and Drug Administration (FDA)-approved drugs. In modern pharmacology of GPCRs, modulating receptor signaling based on requirement of a specific disorder is of immense interest. Classical drugs targeting orthosteric sites in GPCRs completely block the binding of endogenous ligand and consequently inhibit all important signals from a GPCR. Some of many signals elicited by the endogenous ligands may play vital role and inhibiting these may also cause severe side effects in the long run. However, allosteric drugs can modulate GPCR signaling without blocking the endogenous ligand binding. Therefore, allosteric drugs can maintain beneficial signaling of the receptor and prevent unwanted side effects. In this chapter, we will discuss GPCR crystal structures solved with allosteric ligands, advantages of allosteric drugs, and allosteric drugs which are in clinical use or trials.

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