Structure-guided design of peptide-based tryptase inhibitors

被引：25

作者：

McGrath, ME ^{[1
]}

Sprengeler, PA ^{[1
]}

Hirschbein, B ^{[1
]}

Somoza, JR ^{[1
]}

Lehoux, I ^{[1
]}

Janc, JW ^{[1
]}

Gjerstad, E ^{[1
]}

Graupe, M ^{[1
]}

Estiarte, A ^{[1
]}

Venkataramani, C ^{[1
]}

Liu, Y ^{[1
]}

Yee, R ^{[1
]}

Ho, JD ^{[1
]}

Green, MJ ^{[1
]}

Lee, CS ^{[1
]}

Liu, L ^{[1
]}

Tai, V ^{[1
]}

Spencer, J ^{[1
]}

Sperandio, D ^{[1
]}

Katz, BA ^{[1
]}

机构：

[1] Celera Genom Inc, San Francisco, CA 94080 USA

来源：

BIOCHEMISTRY | 2006年 / 45卷 / 19期

关键词：

D O I：

10.1021/bi060173m

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：

Improved peptide- based inhibitors of human, tryptase were discovered using information gleaned from tripeptide library screening and structure- guided design methods, including fragment screening. Our efforts sought to improve this class of inhibitors by replacing the traditional Lys or Arg P1 element. The optimized compounds display low nanomolar potency against the mast cell target and several hundredfold selectivity with respect to serine protease off targets. Thus, replacement of Lys/ Arg at P1 in a peptide-like scaffold does not need to be accompanied by a loss in target affinity.

引用

页码：5964 / 5973

页数：10

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