2. Academic Validation
  3. Potent Triazole Bisphosphonate Inhibitor of Geranylgeranyl Diphosphate Synthase

Potent Triazole Bisphosphonate Inhibitor of Geranylgeranyl Diphosphate Synthase

  • ACS Med Chem Lett. 2015 Oct 28;6(12):1195-8. doi: 10.1021/acsmedchemlett.5b00334.
Veronica S Wills 1,  Cheryl Allen 2,  Sarah A Holstein 2,  David F Wiemer 3
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Iowa , Iowa City, Iowa 52242-1294, United States.
  • 2 Department of Medicine, Roswell Park Cancer Institute , Buffalo, New York 14263, United States.
  • 3 Department of Chemistry, University of Iowa , Iowa City, Iowa 52242-1294, United States ; Department of Pharmacology, University of Iowa , Iowa City, Iowa 52242-1109, United States.
PMID: 26713103 DOI: 10.1021/acsmedchemlett.5b00334
Abstract

Studies of triazole bisphosphonates have resulted in identification of a potent inhibitor of geranylgeranyl diphosphate synthase (IC50 = 45 nM) with very good selectivity for this enzyme over farnesyl diphosphate synthase (IC50 = 28 μM). This compound also potently disrupts geranylgeranylation and induces cytotoxicity in human myeloma cells at submicromolar levels, suggesting that it may serve as a lead compound for treatment of malignancies characterized by excessive protein secretion.

Keywords

GGDPS; Geranylgeranyl diphosphate synthase; bisphosphonate; farnesyl diphosphate synthase; myeloma.

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