Pharmaceuticals | |
Functional Consequences of GPCR Heterodimerization: GPCRs as Allosteric Modulators | |
Karla K.V. Haack1  | |
[1]Department of Cellular and Integrative Physiology, University of Nebraska Medical Center, 985850 Nebraska Medical Center, Omaha, NE 68198, USA | |
[2] E-Mail: | |
关键词: GPCR; heterodimer; allosteric modulator; | |
DOI : 10.3390/ph4030509 | |
来源: mdpi | |
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【 摘 要 】
G Protein Coupled Receptors (GPCRs) represent the largest family of membrane proteins in the human genome, are the targets of approximately 25% of all marketed pharmaceuticals, and the focus of intensive research worldwide given that this superfamily of receptors is as varied in function as it is ubiquitously expressed among all cell types. Increasing evidence has shown that the classical two part model of GPCR signaling (one GPCR, one type of heterotrimeric G protein) is grossly oversimplified as many GPCRs can couple to more than one type of G protein, each subunit of the heterotrimeric G protein can activate different downstream effectors, and, surprisingly, other GPCRs can affect receptor behavior in G protein-independent ways. The concept of GPCR heterodimerization, or the physical association of two different types of GPCRs, presents an unexpected mechanism for GPCR regulation and function, and provides a novel target for pharmaceuticals. Here we present a synopsis of the functional consequences of GPCR heterodimerization in both
【 授权许可】
CC BY
© 2011 by the authors; licensee MDPI, Basel, Switzerland.
【 预 览 】
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