Structural basis for the cyclophilin A binding affinity and immunosuppressive potency of E-ISA247 (voclosporin).

Kuglstatter A; Mueller F; Kusznir EGsell BStihle MThoma RBenz JAspeslet LFreitag DHennig M

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Structural basis for the cyclophilin A binding affinity and immunosuppressive potency of E-ISA247 (voclosporin).

机译：结构性基础还有绑定亲和力和免疫抑制的力量E-ISA247 (voclosporin)。

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E-ISA247 (voclosporin) is a cyclosporin A analogue that is in late-stage clinical development for the treatment of autoimmune diseases and the prevention of organ graft rejection. The X-ray crystal structures of E-ISA247 and its stereoisomer Z-ISA247 bound to cyclophilin A have been determined and their binding affinities were measured to be 15 and 61 nM, respectively, by fluorescence spectroscopy. The higher affinity of E-ISA247 can be explained by superior van der Waals contacts between its unique side chain and cyclophilin A. Comparison with the known ternary structure including calcineurin suggests that the higher immunosuppressive efficacy of E-ISA247 relative to cyclosporin A could be a consequence of structural changes in calcineurin induced by the modified E-ISA247 side chain.

机译：E-ISA247 (voclosporin)是一种环孢菌素类似物后期的临床开发自身免疫性疾病和治疗防止器官移植排斥。E-ISA247及其晶体结构还有立体异构体Z-ISA247绑定到决定和他们的结合亲和力分别测量了15和61海里荧光光谱。由上级范德E-ISA247可以解释瓦尔斯其独特的侧链和之间的联系还有a与已知的三元结构包括钙调磷酸酶表明更高的E-ISA247免疫抑制效果相对于环孢菌素可能是一个结果钙调磷酸酶引起的结构变化修改后的E-ISA247侧链。

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《Acta crystallographica.Section D. Biological crystallography》 |2011年第2期|119-123|共5页
作者
Kuglstatter A; Mueller F; Kusznir EGsell BStihle MThoma RBenz JAspeslet LFreitag DHennig M;
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F. Hoffmann-La Roche, Discovery Technologies, 4070 Basel, Switzerland.;

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正文语种英语
中图分类化学;
关键词
Autoimmune Disease; Calcineurin; Cyclophilin APPIA genebinding affinityfluorescence emission spectroscopyFluorescence SpectroscopyOrgan TransplantsCyclosporins;

机译：自身免疫性疾病;钙调磷酸酶;还有APPIAgenebinding affinityfluorescence发射spectroscopyFluorescence SpectroscopyOrgan;

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Structural basis for the cyclophilin A binding affinity and immunosuppressive potency of E-ISA247 (voclosporin).

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