Design and synthesis of selective inhibitors of placental alkaline phosphatase

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Alkaline Phosphatase / antagonists & inhibitors*
  • Alkaline Phosphatase / metabolism
  • Catechols / chemical synthesis*
  • Catechols / chemistry
  • Catechols / pharmacology*
  • Drug Design*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • GPI-Linked Proteins
  • Isoenzymes / antagonists & inhibitors*
  • Isoenzymes / metabolism
  • Molecular Structure
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Catechols
  • Enzyme Inhibitors
  • GPI-Linked Proteins
  • Isoenzymes
  • Alkaline Phosphatase
  • alkaline phosphatase, placental
  • catechol