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Potent Triazole Bisphosphonate Inhibitor of Geranylgeranyl Diphosphate Synthase.

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 ?M). 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.

SUBMITTER: Wills VS 

PROVIDER: S-EPMC4677368 | biostudies-other | 2015 Dec

REPOSITORIES: biostudies-other

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Potent Triazole Bisphosphonate Inhibitor of Geranylgeranyl Diphosphate Synthase.

Wills Veronica S VS   Allen Cheryl C   Holstein Sarah A SA   Wiemer David F DF  

ACS medicinal chemistry letters 20151028 12

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. ...[more]

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