Signal transmission via G protein-coupled receptors in the light of rhodopsin structure determination.

J Ciarkowski; P Drabik; A Giełdoń; R Kaźmierkiewicz; R Slusarz

doi:10.18388/abp.2001_3892

Signal transmission via G protein-coupled receptors in the light of rhodopsin structure determination.

J Ciarkowski Faculty of Chemistry, University of Gdańsk, Poland. jurek@chemik.chem.univ.gda.pl;
P Drabik
A Giełdoń
R Kaźmierkiewicz
R Slusarz

DOI: https://doi.org/10.18388/abp.2001_3892

Abstract

G protein-coupled receptors (GPCRs) transducing diverse external signals to cells via activation of heterotrimeric GTP-binding (G) proteins, estimated to mediate actions of 60% of drugs, had been resistant to structure determination until summer 2000. The first atomic-resolution experimental structure of a GPCR, that of dark (inactive) rhodopsin, thus provides a trustworthy 3D prototype for antagonist-bound forms of this huge family of proteins. In this work, our former theoretical GPCR models are evaluated against the new experimental template. Subsequently, a working hypothesis regarding the signal transduction mechanism by GPCRs is presented.

Published

2001-12-31

Issue

Vol. 48 No. 4 (2001)

Section

Articles

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