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Design and synthesis of selective inhibitors of Placental Alkaline Phosphatase |
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| Authors: | Marion Lanier Eduard Sergienko Ana Maria Simão Ying Su Thomas Chung José Luis Millán John R. Cashman |
| Affiliation: | 1. Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121-2804, USA;2. Burnham Center for Chemical Genomics, Burnham Institute for Medical Research, 10901 N. Torrey Pines Road, La Jolla, CA 92037, USA;3. Sanford Children’s Health Research Center, Burnham Institute for Medical Research, 10901 N. Torrey Pines Road, La Jolla, CA 92037, USA |
| 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. |
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