Design and Application of a DNA-Encoded Macrocyclic Peptide Library

被引：78

作者：

Zhu, Zhengrong ^{[1
]}

Shaginian, Alex ^{[1
]}

Grady, LaShadric C. ^{[1
]}

O'Keeffe, Thomas ^{[1
]}

Shi, Xiangguo E. ^{[1
]}

Davie, Christopher P. ^{[1
]}

Simpson, Graham L. ^{[2
]}

Messer, Jeffrey A. ^{[1
]}

Evindar, Ghotas ^{[1
]}

Bream, Robert N. ^{[2
]}

Thansandote, Praew P. ^{[2
]}

Prentice, Naomi R. ^{[2
]}

Mason, Andrew M. ^{[2
]}

Pal, Sandeep ^{[2
]}

机构：

[1] GlaxoSmithKline, 200 Cambridge Pk Dr, Cambridge, MA 02140 USA

[2] GlaxoSmithKline, Gunnels Wood Rd, Stevenage SG1 2NY, Herts, England

来源：

ACS CHEMICAL BIOLOGY | 2018年 / 13卷 / 01期

关键词：

PROTEIN-PROTEIN INTERACTION; CHEMICAL LIBRARIES; CYCLIC-PEPTIDES; DRUG DISCOVERY; LEAD DISCOVERY; TECHNOLOGY; ANTAGONISTS; SELECTION; IDENTIFICATION; OPPORTUNITIES;

D O I：

10.1021/acschembio.7b00852

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A DNA-encoded macrocyclic peptide library was designed and synthesized with 2.4 x 10(12) members composed of 4-20 natural and non-natural amino acids. Affinity based selection was performed against two therapeutic targets, VHL and RSV N protein. On the basis of selection data, some peptides were selected for resynthesis without a DNA tag, and their activity was confirmed.

引用

页码：53 / 59

页数：7

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