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

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Ciarkowski J., Drabik P., Giełdoń A., Kaźmierkiewicz R., Ślusarz R.
|
2001
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vol. 48
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issue 4
1203-1207
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.
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