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A Selective Murine Intestinal Alkaline Phosphatase (muIAP) Inhibitor.


Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Oct 31 [updated 2013 Mar 7].


The isozymes of alkaline phosphatase (AP) are capable of dephosphorylation and transphosphorylation of a wide spectrum of substrates in vitro. Their localization in proximity to the cell surface suggests that they help facilitate the movement of substances across the plasma membrane. In humans, four isozymes of APs have been identified - one tissue-nonspecific (TNAP) and three tissue-specific isozymes named according to the tissue of their predominant expression: intestinal (IAP), placental (PLAP) and germ cell (GCAP) alkaline phosphatases. This project sought to identify isozyme and species selective inhibitors and activators of the human and mouse alkaline phosphatases. Concurrent high throughput screening (HTS) campaigns of the NIH Molecular Libraries Small Molecule Repository (MLSMR) library comprising ~355,000 compounds were completed against murine IAP (muIAP), human IAP (huIAP), TNAP and PLAP (TNAP & PLAP are only found in humans) were completed. This Center Probe Report describes the screens and structure activity relationship (SAR) elucidation that led to identification of a potent (540 nM IC50) inhibitor of the murine IAP (muIAP), with 65-fold selectivity against TNAP and >185-fold selectivity against PLAP as well as the human isoform of IAP (huIAP).

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