Design and synthesis of selective inhibitors of Placental Alkaline Phosphatase

被引：30

作者：

Lanier, Marion ^{[1
]}

Sergienko, Eduard ^{[2
]}

Simao, Ana Maria ^{[3
]}

Su, Ying ^{[2
]}

Chung, Thomas ^{[2
]}

Millan, Jose Luis ^{[3
]}

Cashman, John R. ^{[1
]}

机构：

[1] Human BioMol Res Inst, San Diego, CA 92121 USA

[2] Burnham Inst Med Res, Burnham Ctr Chem Genom, La Jolla, CA 92037 USA

[3] Burnham Inst Med Res, Sanford Childrens Hlth Res Ctr, La Jolla, CA 92037 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 02期

关键词：

Enzyme inhibitor; Placental Alkaline Phosphatase; Cancer; Oncodevelopmental; ISOENZYMES; BONE; MINERALIZATION; OSTEOPONTIN; EXPRESSION; LIVER;

D O I：

10.1016/j.bmc.2009.12.012

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：

Placental Alkaline Phosphatase (PLAP) is a tissue-restricted isozyme of the Alkaline Phosphatase (AP) superfamily. PLAP is an oncodevelopmental enzyme expressed during pregnancy and in a variety of human cancers, but its biological function remains unknown. We report here a series of catechol compounds with great affinity for the PLAP isozyme and significant selectivity over other members of the AP superfamily. These selective PLAP inhibitors will provide small molecule probes for the study of the pathophysiological role of PLAP. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：573 / 579

页数：7

共 32 条

[1] Intestinal alkaline phosphatase detoxifies lipopolysaccharide and prevents inflammation in zebrafish in response to the gut microbiota [J].