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Bisphosphonic acids and related compounds as inhibitors of nucleotide‐ and polyphosphate‐processing enzymes: A PPK1 and PPK2 case study
Author(s) -
BurdaGrabowska Małgorzata,
Macegoniuk Katarzyna,
Flick Robert,
Nocek Boguslaw P.,
Joachimiak Andrzej,
Yakunin Alexander F.,
Mucha Artur,
Berlicki Łukasz
Publication year - 2019
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13439
Subject(s) - polyphosphate , pyrophosphate , enzyme , biochemistry , chemistry , nucleotide , combinatorial chemistry , computational biology , biology , gene , phosphate
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 ( PPK 1 and PPK 2). 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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