Bisphosphonic acids and related compounds as inhibitors of nucleotide- and polyphosphate-processing enzymes: A PPK1 and PPK2 case study.

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ID: 97250
2019
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Abstract
Bisphosphonic acids, which are structural analogs of pyrophosphate, constitute a class of compounds with very high potential for the construction of effective inhibitors of enzymes operating on oligo- and polyphosphates. The bisphosphonate-based methodology was applied for the discovery of inhibitors of two families of polyphosphate kinases (PPK1 and PPK2). Screening of thirty-two structurally diverse bisphosphonic acids and related compounds revealed several micromolar inhibitors of both enzymes. Importantly, selectivity of bisphosphonates could be achieved by application of the appropriate side chain.
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burdagrabowska2019bisphosphonicchemical Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Burda-Grabowska, Małgorzata;Macegoniuk, Katarzyna;Flick, Robert;Nocek, Boguslaw P;Joachimiak, Andrzej;Yakunin, Alexander F;Mucha, Artur;Berlicki, Łukasz;
Journal Chemical biology & drug design
Year 2019
DOI
10.1111/cbdd.13439
URL
Keywords
Enzyme inhibitors organophosphorus compounds polyphosphate kinases polyphosphate mimetics

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