Computational Design of a 尾-Peptide That Targets Transmembrane Helices

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• 作者：Scott J. Shandler ; Ivan V. Korendovych ; David T. Moore ; Kathryn B. Smith-Dupont ; Craig N. Streu ; Rustem I. Litvinov ; Paul C. Billings ; Feng Gai ; Joel S. Bennett ; William F. DeGrado
• 刊名：Journal of the American Chemical Society
• 出版年：2011
• 出版时间：August 17, 2011
• 年：2011
• 卷：133
• 期：32
• 页码：12378-12381
• 全文大小：813K
• 年卷期：v.133,no.32(August 17, 2011)
• ISSN：1520-5126

文摘

The design of 尾-peptide foldamers targeting the transmembrane (TM) domains of complex natural membrane proteins has been a formidable challenge. A series of 尾-peptides was designed to stably insert in TM orientations in phospholipid bilayers. Their secondary structures and orientation in the phospholipid bilayer was characterized using biophysical methods. Computational methods were then devised to design a 尾-peptide that targeted a TM helix of the integrin 伪_IIb尾₃. The designed peptide (尾-CHAMP) interacts with the isolated target TM domain of the protein and activates the intact integrin in vitro.