Effect of mutation of Phe 2436.44 of the histamine H2 receptor on cimetidine and ranitidine mechanism of action.

Abstract excerpt

Despite the pivotal role GPCRs play in cellular signaling, it is only in the recent years that structural biology has begun to elucidate how GPCRs function and to provide a platform for structure-based drug design. It is postulated that GPCR activation involves the movement of transmembrane helices. The finding that many residues, which have been shown to be critical for receptor activation and are highly...

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