title: Synthesis and screening of small-molecule α-helix mimetic libraries targeting protein-protein interactions.
abstract: α-Helices are the most common protein secondary structure and play a key role in mediating many protein-protein interactions (PPIs) by serving as recognition motifs. Given that aberrant α-helix-mediated PPIs are linked to various disease states, targeting such interactions with small-molecules represents an attractive strategy to develop therapeutic candidates for the related diseases. Over the last decade, significant efforts have been directed toward developing α-helix mimetic small-molecules that can modulate α-helix-mediated PPIs. In this review, we will highlight recent advances in the development of non-peptidic, small-molecule α-helix mimetics with a focus on library synthesis and screening methods to efficiently discover small-molecule α-helix mimetics.
authors.affiliation: Department of Chemistry, Pohang University of Science and Technology, Pohang 790-784, South Korea.
authors.forename: Heejo
authors.initials: H
authors.lastname: Moon
authors.affiliation: Department of Chemistry, Pohang University of Science and Technology, Pohang 790-784, South Korea; Department of Biochemistry and Molecular Biology, Indiana University School of Medicine, Indianapolis, IN 46032, United States. Electronic address: hslim@postech.ac.kr.
authors.forename: Hyun-Suk
authors.initials: HS
authors.lastname: Lim
mesh_terms: D000818:Animals; D032701:Biomimetics / Q000379:methods*; D060326:Chemistry Techniques, Synthetic / Q000379:methods; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D060066:Protein Interaction Maps / Q000187:drug effects*; D017433:Protein Structure, Secondary; D011506:Proteins / Q000737:chemistry / Q000378:metabolism; D054852:Small Molecule Libraries / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D011506:Proteins; D054852:Small Molecule Libraries