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双膦酸盐类化合物的研究进展 被引量：5

Recent advance of the study on bisphosphonates
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摘要 双膦酸盐类化合物是防治骨代谢疾病的重要药物 ,本文对双膦酸盐类药物的临床应用、构效关系、作用机制进行了综述 。 Bisphosphonates are important class of antiresorptive agents used in the treatment of various bone mineral metabolism disorders.This article reviews the development,clinicalapplication,QSAR studies of bisphosphonates,and describes recent new discoveries of their molecular mechanism of action in osteoclast.
作者 徐广宇 谢毓元
机构地区 中国科学院上海药物研究所
出处 《中国药物化学杂志》 CAS CSCD 2004年第3期182-186,共5页 Chinese Journal of Medicinal Chemistry
关键词 药物化学 综述 双膦酸盐 临床应用 构效关系 分子作用机制 法呢基焦磷酸酯合成酶 medicinal chemistry review bisphosphonates clinical application QSAR molecular mechanism farnesyl pyrophosphonate synthase
分类号 R98 [医药卫生—药品]
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参考文献34

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  • 2Dunford JE,Thompson K,Coxon FP,et al.Relationships for inhibition offarnesyl diphosphonate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates[J].J Pharm Exp Ther,2001,296(2):235-242.
  • 3Kotsikorou E,Oldfield E.A quantitative structure-activity relationship and pharmacophore modeling investigation of aryl-X and heterocyclic bisphosphonates as bone resorption agents[J].J Med Chem,2003,46(14):2932-2944.
  • 4Benford HL,Frith JC,Auriola S,et al.Farnesol and geranylgeraniol prevent activation of caspases by aminobisphosphonates:biochemical evidence for twodistinct pharmacological classes of bisphosphonate drugs[J].Mol Pharmacol,1999,56(1):131-140.
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  • 6Frith JC,Monkkonen J,Blackburn GM,et al.Clodronate and liposome-encapsulated clodronate are metabolized to a toxic ATP analogue,adenosine 5′-(beta,gamma-dichloromethylene)triphosphate,by mammalian cells in vitro[J].J Bone Miner Res,1997,12(9):1358-1367.
  • 7Lehenkari PP,Kellinsalmi M,Napankangas JP,et al.Further insight intomechanism of action of clodronate:inhibition of mitochondrial ADP/ATP translocase by a nonhydrolyzable,adenine-containing metabolite[J].Mol Pharmacol,2002,61(5):1255-1262.
  • 8Luckman SP,Hughes DE,Coxon FP,et al.Nitrogen-containing bisphosphonates inhibit the mevalonate pathway and prevent post-translational prenylation of GTP-binding proteins,including Ras[J].J Bone Miner Res,1998,13(4):581-589.
  • 9Fisher JE,Rogers MJ,Halasy JM,et al.Alendronate mechanism of action:geranylgeraniol,an intermediate in the mevalonate pathway,prevents inhibition ofosteoclast formation,bone resorption and kinase activation in vitro[J].Proc Natl Acad Sci,1999,96(1):133-13
  • 10Van Beek E,Lowik,van der Pluijm G,et al.The role of geranylgeranylation in bone resorption and its suppression by bisphosphonates in fetal bone explants in vitro:a clue to the mechanism of action of nitrogen-containing bisphosphonates[J].J Bone Miner Res,

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中国药物化学杂志
2004年 第3期

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