{Reference Type}: Journal Article
{Title}: Bisphosphonic acids and related compounds as inhibitors of nucleotide- and polyphosphate-processing enzymes: A PPK1 and PPK2 case study.
{Author}: Burda-Grabowska M;Macegoniuk K;Flick R;Nocek BP;Joachimiak A;Yakunin AF;Mucha A;Berlicki Ł;
{Journal}: Chem Biol Drug Des
{Volume}: 93
{Issue}: 6
{Year}: 06 2019
{Factor}: 2.873
{DOI}: 10.1111/cbdd.13439
{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.