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

• Authors: Jerzy Ciarkowski , Piotr Drabik , Artur Giełdoń , Rajmund Kaźmierkiewicz , Rafał Ślusarz
• Languages of publication: EN

Abstracts

EN

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.

Keywords

EN

signal transduction; neurohypophyseal receptors; molecular modeling; GPCRs

• Publisher: Polish Biochemical Society
• Journal: Acta Biochimica Polonica
• Year: 2001
• Volume: 48
• Issue: 4
• Pages: 1203-1207

Dates

published

2001

received

2001-10-17

accepted

2001-11-12

Contributors

author

Jerzy Ciarkowski

• Faculty of Chemistry, University of Gdańsk, Gdańsk, Poland

author

Piotr Drabik

• Department of Public Health, University School of Physical Education, Gdańsk, Poland

author

Artur Giełdoń

• Faculty of Chemistry, University of Gdańsk, Gdańsk, Poland

author

Rajmund Kaźmierkiewicz

• Faculty of Chemistry, University of Gdańsk, Gdańsk, Poland

author

Rafał Ślusarz

• Faculty of Chemistry, University of Gdańsk, Gdańsk, Poland

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