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Lifitegrast合成路线图解 被引量：1

Graphical Synthetic Routes of Lifi tegrast
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摘要 Lifitegrast（1）,化学名为（S）-2-[2-（苯并呋喃-6-羰基）-5,7-二氯-1,2,3,4-四氢异喹啉-6-甲酰胺基]-3-（3-甲磺酰基苯基）丙酸（1）,是美国Sunesis公司开发的一种用于治疗成人患者干眼症的药物,目前在美国处于注册前阶段。在干眼病中,细胞间黏附分子-1（ICAM-1）在角膜和结膜组织中过量表达。1是一种新型的小分子整合素抑制剂,
作者 张利军 梁慧兴 张海波
机构地区 扬子江药业集团有限公司
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2016年第4期493-496,共4页 Chinese Journal of Pharmaceuticals
关键词 异喹啉 磺酰基 苯并呋喃 成人患者 细胞间黏附分子 干眼病 Lifitegrast 过量表达 结膜组织 丙酸苄酯
分类号 R988.1 [医药卫生—药品]
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参考文献12

  • 1Zhong M, Hanan EJ, Shen W, et al. Structure-activity relationship (SAR) of the ct-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA- 1/ICAM-1 antagonists [J]. BioorgMed Chem Lett, 2011, 21: 307-310.
  • 2李猛,高春记.LFA-1与配体ICAM-1黏附分子功能的研究进展[J].中国实验血液学杂志,2008,16(1):213-216. 被引量：15
  • 3Min Z, Thomas R, Gadek MB, et al. Discovery anddevelopment of potent LFA- 1/ICAM- 1 antagonist SAR1118 as an ophthalmic solution for treating dry eye [J]. ACS Med Chem Lett, 2012, 3: 203-206.
  • 4Zeller J, Venkatrman S, Brot E, et al. LFA-1 inhibitor and polymorph thereof: WO, 2014018748A1 [P]. 2014-01-30.
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  • 6泽勒瓜,文卡特拉曼S,布罗特ECA,等.LFA-1抑制剂及其多晶型物:中国,104797574A[P].2015-07-22.
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二级参考文献25

  • 1Shamri R, Grabovsky V, Gauguet JM, et al. Lymphocyte arrest requires instantaneous induction of an extended LFA-1 conformation mediated by endothelium-bound chemokines. Nat Immunol, 2005 ; 6:497-506.
  • 2Smith A, Carrasco YR, Stanley P, et al. A talin-dependent LFA-1 focal zone is formed by rapidly migrating T lymphocytes. J Cell Biol. 2005; 170:141-151.
  • 3Mould AP, Humphries MJ. Regulation of integrin function through conformational complexity: not simply a knee-jerk reaction? Curr Opin Cell Biol. 2004 ; 16:544-551.
  • 4Jo EK, Wang H, Rudd CE. An essential role for SKAP-55 in LFA-1 clustering on T cells that cannot be substituted by SKAP55R. J Exp Med. 2005 ; 201:1733-1739.
  • 5Kim M, Carman CV, Yang W, et al. The primacy of affinity over clustering in regulation of adhesiveness of the integrin αLβ2. J Cell Biol,2004 ; 167 : 1241-1253.
  • 6Sarantos MR, Raychaudhuri S, Lum AF, et al. Leukocyte function-associated antigen 1-mediated adhesion stability is dynamically regulated through affinity and valency during bond formation with intercellular adhesion molecule-1. J Biol Chem; 2005, 280:28290-28298.
  • 7Pepper LR, Hammer DA, Boder ET. Rolling Adhesion of αLI Domain Mutants Decorrelated from Binding Affinity. J Mol Biol, 2006; 360:37-44.
  • 8Cambi A, Joosten B, Koopman M, et al. Organization of the integrin LFA-1 in nanoclusters regulates its activity. Mol Biol Cell, 2006;10:4270-4281.
  • 9Zheng Y, Liu H, Coughlin J, et al. Phosphorylation of RasGRP3 on threonine 133 provides a mechanistic link between PKC and Ras signaling systems in B cells. Blood, 2005; 105:3648-3654.
  • 10Dustin ML, Bivona TG, Philips MR. Membrane as messengers in T cell adhesion singnaling. Nat Immunl, 2004 ; 5 : 363-370.

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中国医药工业杂志
2016年 第4期

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