Cyclophilin inhibitors: a novel class of promising host-targeting anti-HCV agents.
Cyclophilin inhibitors: a novel class of promising host-targeting anti-HCV agents.
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DOI：
10.1007/s12026-011-8263-5
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发表时间：
2012-06
影响因子：
4.4
通讯作者：
Gallay PA
中科院分区：
文献类型：
--
作者：
Gallay PA
随着2011年批准的蛋白酶抑制剂Victrelis和Incivek，直接作用抗病毒药物(DAA)已开始革命性的丙型肝炎病毒的治疗。尽管在聚乙二醇化干扰素α和利巴韦林(p干扰素α/rbv)的基础上加用因西韦克或维特瑞斯，可能会提高治愈率并缩短“旧”护理标准(SOC)的治疗时间，但这种三联疗法不适用于对p干扰素α或rbv不耐受的患者。这种三联疗法的疗效肯定也会在p干扰素α/RBV无应答者中减弱。由于Incivek对基因3型(Gt3)无效，加上所有的蛋白酶抑制剂和大多数正在开发的非核苷类聚合酶抑制剂主要对Gt1起作用，因此在新类型的抑制剂进入临床实践之前，pIFNα/RBV仍将是非Gt1的SOC。对这种新的三联疗法没有反应的GT1患者将对蛋白酶抑制剂产生抗药性，这将限制未来的治疗选择。因此，有必要鉴定新的有效的丙型肝炎病毒制剂。最近出现了一类具有巨大治疗潜力的新型丙型肝炎病毒抑制剂：宿主靶向抗病毒药物(HTA)亲环素(Cyp)抑制剂。
With the approval in 2011 of the protease inhibitors Victrelis and Incivek, direct-acting antivirals (DAA) have begun to revolutionize HCV treatment. Although the addition of Incivek or Victrelis to PEGylated IFNα and ribavarin (pIFNα/RBV) may improve cure rates and shorten the treatment duration of the “old” standard of care (SOC), this triple therapy will not be suitable for patients intolerant to pIFNα or RBV. The efficacy of this triple therapy will also certainly be attenuated in pIFNα/RBV non-responders. As Incivek is inactive against genotype 3 (GT3) combined with the fact that all protease inhibitors and most of the non-nucleoside polymerase inhibitors in development are active primarily against GT1, pIFNα/RBV will remain the SOC for non-GT1 until new classes of inhibitors enter into clinical practice. GT1 patients, who do not respond to this new triple therapy will have developed resistance to protease inhibitors that will limit future treatment options. There is thus an important need for the identification of new potent HCV agents. A novel class of HCV inhibitors that have great potential for the treatment of HCV has recently emerged: the host-targeting antivirals (HTA) cyclophilin (Cyp) inhibitors.
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影响因子：
3.7
作者：
Coelmont L;Hanoulle X;Chatterji U;Berger C;Snoeck J;Bobardt M;Lim P;Vliegen I;Paeshuyse J;Vuagniaux G;Vandamme AM;Bartenschlager R;Gallay P;Lippens G;Neyts J
通讯作者：
Neyts J
影响因子：
13.5
作者：
Flisiak, Robert;Horban, Andrzej;Scalfaro, Pietro
通讯作者：
Scalfaro, Pietro
影响因子：
11.4
作者：
Braaten, D;Luban, J
通讯作者：
Luban, J
影响因子：
29.4
作者：
Foster, Graham R.;Hezode, Christophe;Beumont, Maria
通讯作者：
Beumont, Maria
影响因子：
158.5
作者：
DAVIS, GL;BALART, LA;GIBAS, A
通讯作者：
GIBAS, A