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Biochim Biophys Acta. 1999 Nov 16;1422(3):207-34.

Modelling G-protein-coupled receptors for drug design.

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  • Department of Physical Sciences, ASTRA Charnwood, Bakewell Rd, Loughborough, Leicestershire, UK. flower@jenner.ac.uk


The G-protein coupled receptors form a large and diverse multi-gene superfamily with many important physiological functions. As such, they have become important targets in pharmaceutical research. Molecular modelling and site-directed mutagenesis have played an important role in our increasing understanding of the structural basis of drug action at these receptors. Aspects of this understanding, how these techniques can be used within a drug-design programme, and remaining challenges for the future are reviewed.

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