设计和合成胎盘碱性磷酸酶的选择性抑制剂。
Design and synthesis of selective inhibitors of placental alkaline phosphatase.
机构信息
Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121-2804, USA.
出版信息
Bioorg Med Chem. 2010 Jan 15;18(2):573-9. doi: 10.1016/j.bmc.2009.12.012. Epub 2009 Dec 11.
Abstract
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.
摘要
胎盘碱性磷酸酶（PLAP）是碱性磷酸酶（AP）超家族的一种组织特异性同工酶。PLAP 是一种在妊娠期间和多种人类癌症中表达的肿瘤发育酶，但它的生物学功能尚不清楚。我们在这里报告了一系列对 PLAP 同工酶具有高亲和力的儿茶酚化合物，并且对 AP 超家族的其他成员具有显著的选择性。这些选择性 PLAP 抑制剂将为研究 PLAP 的病理生理作用提供小分子探针。
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