Photo-affinity labeling strategy to study the binding site of G protein-coupled receptors

doi:10.1007/s11458-011-0245-6

Front Chem Chin

2011, Vol. 6

Issue (3) : 200-205 https://doi.org/10.1007/s11458-011-0245-6

REVIEW ARTICLE

Photo-affinity labeling strategy to study the binding site of G protein-coupled receptors

Yihui CHEN(

)

Beijing Laviana Pharmatech Co., Ltd., Beijing 102206, China

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Abstract

G protein-coupled receptors (GPCRs) are involved in the control of every aspect of our behavior and physiology. GPCR can be involved in pathological processes as well and are linked to numerous diseases, including cardiovascular and mental disorders, retinal degeneration, cancer, and AIDS. This article reviews the methods of approaching photo-affinity labeling strategy to obtain the possible G protein-coupled receptors’s binding site.

Keywords GPCR photo-affinity labeling rhodopsin transmembrane structure binding

Corresponding Author(s): CHEN Yihui,Email:yihuichen@lavianacorp.com

Issue Date: 05 September 2011

Cite this article:

Yihui CHEN. Photo-affinity labeling strategy to study the binding site of G protein-coupled receptors[J]. Front Chem Chin, 2011, 6(3): 200-205.

URL:

https://academic.hep.com.cn/fcc/EN/10.1007/s11458-011-0245-6
https://academic.hep.com.cn/fcc/EN/Y2011/V6/I3/200

Fig.1 Photo-affinity labeling principle and the steps to identify the fine structure information

Fig.2 Scheme 1 Several photo-affinity labeling groups used as precursors

Fig.3 Scheme 2 Photochemistry of benzopheone chromophore and redical recombination pathways

Fig.4 Interface between the heterotrimeric G protein transducin and its receptor rhodopsin. Transducin (1GOT) consists of the nucleotide binding Gtα subunit and the heterodimeric Gtβγ subunit binding sites for transducin on the GPCR rhodopsin (1HL9), which contains the bound chromophore 11--retinal (, space-filling model).

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