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A Trp in chi space
Authors:DC Horwell  MJ McKiernan  D Naylor and SA Osborne
Institution:(1) Parke-Davis Neuroscience Research Centre, Cambridge University, Forvie Site, Robinson Way, Cambridge, CB2 2QB, U.K.;(2) Present address: Faculté de Pharmacie, 15 Avenue Charles Flahault, 34060 Montpellier, Cedex, France
Abstract:Our aim is to identify and synthesise a lsquofamilyrsquo of tryptophan mimetics which thoroughly explore chi space and then incorporate them into selected ligands for biological receptors e.g. Tachykinin NK1. This project is considered important as only the psgr-phgr angles have previously been explored; obtaining a greater understanding of the spacial orientation of the side chain in chi space (chi1-chi2) should prove invaluable to the future design of peptidomimetics. The amino acid tryptophan was selected as it has proved pivotal in many pharmaceutic drug programmes.
Keywords:bombesin  cholecystokinin  conformational constraints  novel tryptophan derivatives  tachykinin
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