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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Non-Peptidic α-Helical Mimetics as Protein-Protein Interaction Inhibitors

Author(s): M. B. Dewal and S. M. Firestine

Volume 18, Issue 16, 2011

Page: [2420 - 2428] Pages: 9

DOI: 10.2174/092986711795843227

Price: $65


Protein-protein interactions play a major role in almost all biological pathways and thus, these interactions have a profound impact on the pathogenesis of diseases. The ability to modulate protein-protein interactions with small molecules is an important and rapidly growing area in the field of medicinal chemistry. One of the most common secondary protein structures that are involved in protein-protein interactions are α-helices. Thus, a common approach towards developing inhibitors of protein-protein interactions is to design non-peptidic small molecules that mimic the spatial orientations of the side chains of an α-helix. In this review, we will discuss a variety of small molecules including terephenyls, terephthalamides, benzamides, enaminones, benzoylureas, pyridines, imidazoles, thiazoles, pyridazines, piperazines, oxopiperazines and diphenylindanes that have been published from 2005-2010 as small molecule α- helical mimetics.

Keywords: α-helical mimetics, protein-protein interactions, benzoylurea, enaminone, non-peptidic, oxopiperazine, terephenyls, terephthalamides, heterocycles, benzamide, pyridazine, amphiphilic, hydrogen bond, hydrophilic

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