title: Design and synthesis of selective inhibitors of placental alkaline phosphatase.
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.
authors.affiliation: Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121-2804, USA. mlanier@hbri.org
authors.forename: Marion
authors.initials: M
authors.lastname: Lanier
authors.forename: Eduard
authors.initials: E
authors.lastname: Sergienko
authors.forename: Ana Maria
authors.initials: AM
authors.lastname: Simão
authors.forename: Ying
authors.initials: Y
authors.lastname: Su
authors.forename: Thomas
authors.initials: T
authors.lastname: Chung
authors.forename: José Luis
authors.initials: JL
authors.lastname: Millán
authors.forename: John R
authors.initials: JR
authors.lastname: Cashman
mesh_terms: D000469:Alkaline Phosphatase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D002396:Catechols / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D058851:GPI-Linked Proteins; D007527:Isoenzymes / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D002396:Catechols; D004791:Enzyme Inhibitors; D058851:GPI-Linked Proteins; D007527:Isoenzymes; D000469:Alkaline Phosphatase; C019839:alkaline phosphatase, placental; C034221:catechol