Journal article
Potent Triazole Bisphosphonate Inhibitor of Geranylgeranyl Diphosphate Synthase
ACS Medicinal Chemistry Letters, Vol.6(12), pp.1195-1198
2015
DOI: 10.1021/acsmedchemlett.5b00334
PMCID: PMC4677368
PMID: 26713103
Abstract
Studies of triazole bisphosphonates have resulted in identification of a potent inhibitor of geranylgeranyl diphosphate synthase (IC 50 = 45 nM) with very good selectivity for this enzyme over farnesyl diphosphate synthase (IC 50 = 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.
Details
- Title: Subtitle
- Potent Triazole Bisphosphonate Inhibitor of Geranylgeranyl Diphosphate Synthase
- Creators
- Veronica S Wills - University of IowaCheryl Allen - Roswell Park Cancer InstituteSarah A Holstein - Roswell Park Cancer InstituteDavid F Wiemer - University of Iowa
- Resource Type
- Journal article
- Publication Details
- ACS Medicinal Chemistry Letters, Vol.6(12), pp.1195-1198
- DOI
- 10.1021/acsmedchemlett.5b00334
- PMID
- 26713103
- PMCID
- PMC4677368
- NLM abbreviation
- ACS Med Chem Lett
- ISSN
- 1948-5875
- eISSN
- 1948-5875
- Publisher
- American Chemical Society
- Grant note
- DOI: 10.13039/100000054, name: U.S. Department of Health and Human Services, award: R01CA-172070, T32 GM008365; DOI: 10.13039/100001024, name: Roy J. Carver Charitable Trust; DOI: 10.13039/100001422, name: American Society of Hematology
- Language
- English
- Date published
- 2015
- Academic Unit
- Neuroscience and Pharmacology; Chemistry
- Record Identifier
- 9983985825502771
Metrics
20 Record Views