Synthesis and Conformation-Activity Relationships of the Peptide Isosteres of FK228 and Largazole

被引：95

作者：

Bowers, Albert A. ^{[3
]}

Greshock, Thomas J. ^{[3
]}

West, Nathan ^{[4
,5
]}

Estiu, Guillermina ^{[1
]}

Schreiber, Stuart L. ^{[5
,6
]}

Wiest, Olaf ^{[1
]}

Williams, Robert M. ^{[2
,3
]}

Bradner, James E. ^{[4
,5
]}

机构：

[1] Univ Notre Dame, Dept Chem & Biochem, Notre Dame, IN 46556 USA

[2] Univ Colorado, Ctr Canc, Aurora, CO 80045 USA

[3] Colorado State Univ, Dept Chem, Ft Collins, CO 80523 USA

[4] Dana Farber Canc Inst, Div Hematol Neoplasia, Boston, MA 02115 USA

[5] Broad Inst Harvard & MIT, Chem Biol Program, Cambridge, MA 02142 USA

[6] Harvard Univ, Howard Hughes Med Inst, Cambridge, MA 02138 USA

来源：

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY | 2009年 / 131卷 / 08期

基金：

英国惠康基金;

关键词：

HISTONE DEACETYLASE INHIBITORS; CHROMOBACTERIUM-VIOLACEUM NO-968; AZUMAMIDE-A; POTENT; DEPSIPEPTIDE; FR901228; DESIGN; TRICHOSTATIN; TRAPOXIN; DOCKING;

D O I：

10.1021/ja807772w

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The peptide isosteres (110 and 11) of the naturally occurring and potent histone deacetylase (HDAC) inhibitors FK228 and largazole have been synthesized and evaluated side-by-side with FK228, largazole, and SAHA for inhibition of the class I HDACs 1, 2, 3, and 6.

引用

页码：2900 / 2905

页数：6

共 33 条

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