α-Helix mimetics: Outwards and upwards

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:24

Article

Jayatunga, Madura K. P.¹  Thompson, Sam¹  Hamilton, Andrew D.¹ 

[1] Univ Oxford, Dept Chem, Chem Res Lab, Oxford OX1 3TA, England

关键词: Protein-protein interaction;    Rational design;    Peptidomimetic;    Proteomimetic;   

DOI  :  10.1016/j.bmcl.2013.12.003

来源: Elsevier

【 摘 要 】

alpha-Helices are common secondary structural elements forming key parts of the large, generally featureless interfacial regions of many therapeutically-relevant protein-protein interactions (PPIs). The rational design of helix mimetics is an appealing small-molecule strategy for the mediation of aberrant PPIs, however the first generation of scaffolds presented a relatively small number of residues on a single recognition surface. Increasingly, helices involved in PPIs are found to have more complex binding modes, utilizing two or three recognition surfaces, or binding with extended points of contact. To address these unmet needs the design and synthesis of new generations of multi-sided, extended, and supersecondary structures are underway. (C) 2013 The Authors. Published by Elsevier Ltd. All rights reserved.

【 授权许可】

Free