Fersiynau electronig

Dangosydd eitem ddigidol (DOI)

  • Małgorzata Burda-Grabowska
    Wrocław University of Science and Technology
  • Katarzyna Macegoniuk
    Wrocław University of Science and Technology
  • Robert Flick
    University of Toronto
  • Boguslaw P Nocek
    Midwest Center for Structural Genomics and Structural Biology Center
  • Andrzej Joachimiak
    Midwest Center for Structural Genomics and Structural Biology Center
  • Alexander F Yakunin
    University of Toronto
  • Artur Mucha
    Wrocław University of Science and Technology
  • Łukasz Berlicki
    Wrocław University of Science and Technology

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.

Allweddeiriau

Iaith wreiddiolSaesneg
Tudalennau (o-i)1197-1206
Nifer y tudalennau10
CyfnodolynChemical biology & drug design
Cyfrol93
Rhif y cyfnodolyn6
Dyddiad ar-lein cynnar28 Tach 2018
Dynodwyr Gwrthrych Digidol (DOIs)
StatwsCyhoeddwyd - 1 Meh 2019
Cyhoeddwyd yn allanolIe
Gweld graff cysylltiadau