Ontology highlight
ABSTRACT:
SUBMITTER: Zhang Y
PROVIDER: S-EPMC2753403 | biostudies-literature | 2009 Apr
REPOSITORIES: biostudies-literature
Zhang Yonghui Y Cao Rong R Yin Fenglin F Hudock Michael P MP Guo Rey-Ting RT Krysiak Kilannin K Mukherjee Sujoy S Gao Yi-Gui YG Robinson Howard H Song Yongcheng Y No Joo Hwan JH Bergan Kyle K Leon Annette A Cass Lauren L Goddard Amanda A Chang Ting-Kai TK Lin Fu-Yang FY Van Beek Ermond E Papapoulos Socrates S Wang Andrew H-J AH Kubo Tadahiko T Ochi Mitsuo M Mukkamala Dushyant D Oldfield Eric E
Journal of the American Chemical Society 20090401 14
Considerable effort has focused on the development of selective protein farnesyl transferase (FTase) and protein geranylgeranyl transferase (GGTase) inhibitors as cancer chemotherapeutics. Here, we report a new strategy for anticancer therapeutic agents involving inhibition of farnesyl diphosphate synthase (FPPS) and geranylgeranyl diphosphate synthase (GGPPS), the two enzymes upstream of FTase and GGTase, by lipophilic bisphosphonates. Due to dual site targeting and decreased polarity, the comp ...[more]