Document Report Card

Basic Information

ID: ALA3774363

Journal: ACS Med Chem Lett

Title: Potent Triazole Bisphosphonate Inhibitor of Geranylgeranyl Diphosphate Synthase.

Authors: Wills VS, Allen C, Holstein SA, Wiemer DF.

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.

CiteXplore: 26713103

DOI: 10.1021/acsmedchemlett.5b00334