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Allosteric Modulation of the Dopamine Receptor by...
Journal article

Allosteric Modulation of the Dopamine Receptor by Conformationally Constrained Type VI β-Turn Peptidomimetics of Pro-Leu-Gly-NH2

Abstract

A peptidomimetic of Pro-Leu-Pro-NH2, 7, possessing an indolizidinone type VI beta-turn mimic was synthesized via improved high-yielding protocols for the preparation and Cbz protection of alpha-allylproline. Bicyclic peptidomimetic 7 and spirobicylic peptidomimetic 8 enhanced the binding of [3H] N-propylnorapomorphine to dopamine receptors indicating that a type VI beta-turn is a possible bioactive conformation of the homochiral Pro-Leu-Pro-NH2 …

Authors

Vartak AP; Skoblenick K; Thomas N; Mishra RK; Johnson RL

Journal

Journal of Medicinal Chemistry, Vol. 50, No. 26, pp. 6725–6729

Publisher

American Chemical Society (ACS)

Publication Date

December 27, 2007

DOI

10.1021/jm070895r

ISSN

0022-2623