ReviewMolecules (Basel, Switzerland)2010
Assay format as a critical success factor for identification of novel inhibitor chemotypes of tissue-nonspecific alkaline phosphatase from high-throughput screening.
Review in Molecules (Basel, Switzerland), 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 22 citations in OpenAlex.
- Tricyclic coumarin sulphonate derivatives with alkaline phosphatase inhibitory effects: in vitro and docking studies.Journal of enzyme inhibition and medicinal chemistry · 2018Article
- Design, synthesis and evaluation of benzoisothiazolones as selective inhibitors of PHOSPHO1.Bioorganic & medicinal chemistry letters · 2014Article
- Identification of a selective inhibitor of murine intestinal alkaline phosphatase (ML260) by concurrent ultra-high throughput screening against human and mouse isozymes.Bioorganic & medicinal chemistry letters · 2014Article
- Pharmacological inhibition of PHOSPHO1 suppresses vascular smooth muscle cell calcification.Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research · 2013Article
- Hypophosphatasia - pathophysiology and treatment.Actualizaciones en osteologia · 2012Article
- Characterization of phosphate solubilizing bacteria in sediments from a shallow eutrophic lake and a wetland: isolation, molecular identification and phosphorus release ability determination.Molecules (Basel, Switzerland) · 2010Article
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Authors and funding
3 authors at 1 institution in 1 country.
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Abstract
The tissue-nonspecific alkaline phosphatase (TNAP) isozyme is centrally involved in the control of normal skeletal mineralization and pathophysiological abnormalities that lead to disease states such as hypophosphatasia, osteoarthritis, ankylosis and vascular calcification. TNAP acts in concert with the nucleoside triphosphate pyrophosphohydrolase-1 (NPP1) and the Ankylosis protein to regulate the extracellular concentrations of inorganic pyrophosphate (PP(i)), a potent inhibitor of mineralization. In this review we describe the serial development of two miniaturized high-throughput screens (HTS) for TNAP inhibitors that differ in both signal generation and detection formats, but more critically in the concentrations of a terminal alcohol acceptor used. These assay improvements allowed the rescue of the initially unsuccessful screening campaign against a large small molecule chemical library, but moreover enabled the discovery of several unique classes of molecules with distinct mechanisms of action and selectivity against the related placental (PLAP) and intestinal (IAP) alkaline phosphatase isozymes. This illustrates the underappreciated impact of the underlying fundamental assay configuration on screening success, beyond mere signal generation and detection formats.
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