Literature DB >> 20544107

Discovery of potent inhibitor for farnesyl pyrophosphate synthase in the mevalonate pathway.

Jinbo Gao1, Xiusheng Chu, Yongge Qiu, Long Wu, Yuqin Qiao, Jiasheng Wu, Ding Li.   

Abstract

The mevalonate pathway is an important drug target for the treatment of cancer and cardiovascular disease. We synthesized and studied a new type of nitrogen-containing bisphosphonate analogs and developed a sensitive end point assay method for enzyme FPPS, which was used for inhibitor screening. One potent FPPS inhibitor was discovered, and the structure-activity relationship of bisphosphonates for the enzyme inactivation was studied.

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Year:  2010        PMID: 20544107     DOI: 10.1039/c0cc00992j

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN: 1359-7345            Impact factor:   6.222


  2 in total

1.  An enzyme-coupled continuous fluorescence assay for farnesyl diphosphate synthases.

Authors:  Jonathan K Dozier; Mark D Distefano
Journal:  Anal Biochem       Date:  2011-10-28       Impact factor: 3.365

2.  The isoprenoid derivative N6 -benzyladenosine CM223 exerts antitumor effects in glioma patient-derived primary cells through the mevalonate pathway.

Authors:  Elena Ciaglia; Manuela Grimaldi; Mario Abate; Mario Scrima; Manuela Rodriquez; Chiara Laezza; Roberta Ranieri; Simona Pisanti; Pierangela Ciuffreda; Clementina Manera; Patrizia Gazzerro; Anna Maria D'Ursi; Maurizio Bifulco
Journal:  Br J Pharmacol       Date:  2017-06-11       Impact factor: 8.739

  2 in total

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