Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling

被引：0

作者：

Petrova, Elissaveta ^{[1
,2
]}

Rios-Esteves, Jessica ^{[1
,3
]}

Ouerfelli, Ouathek ^{[4
]}

Glickman, J. Fraser ^{[5
]}

Resh, Marilyn D. ^{[1
,3
,6
,7
]}

机构：

[1] Mem Sloan Kettering Canc Ctr, Cell Biol Program, New York, NY 10021 USA

[2] Cornell Univ, Grad Program Pharmacol, Weill Cornell Grad Sch Med Sci, New York, NY 10021 USA

[3] Mem Sloan Kettering Canc Ctr, Gerstner Sloan Kettering Grad Sch Biomed Sci, New York, NY 10021 USA

[4] Mem Sloan Kettering Canc Ctr, Pharmacol Program, New York, NY 10021 USA

[5] Rockefeller Univ, High Throughput Screening Resource Ctr, New York, NY 10021 USA

[6] Cornell Univ, Weill Cornell Grad Sch Med Sci, Grad Program Cell Biol, New York, NY 10021 USA

[7] Cornell Univ, Weill Cornell Grad Sch Med Sci, Grad Program Biochem, New York, NY 10021 USA

来源：

NATURE CHEMICAL BIOLOGY | 2013年 / 9卷 / 04期

基金：

美国国家卫生研究院;

关键词：

SMALL-MOLECULE; FATTY-ACIDS; PALMITOYLATION; ACTIVATION; PROTEINS; CELLS;

D O I：

10.1038/NCHEMBIO.1184

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：

Inhibition of Sonic hedgehog (Shh) signaling is of great clinical interest. Here we exploit Hedgehog acyltransferase (Hhat)-mediated Shh palmitoylation, a modification critical for Shh signaling, as a new target for Shh pathway inhibition. A target-oriented high-throughput screen was used to identify small-molecule inhibitors of Hhat. In cells, these Hhat inhibitors specifically block Shh palmitoylation and inhibit autocrine and paracrine Shh signaling.

引用

页码：247 / 249

页数：3

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