Retrocyclins and their activity against HIV-1.
Retrocyclins and their activity against HIV-1.
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DOI：
10.1007/s00018-011-0715-5
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发表时间：
2011-07
期刊：
影响因子：
--
通讯作者：
Cole AM
中科院分区：
文献类型：
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作者：
Penberthy WT;Chari S;Cole AL;Cole AM
灵长类θ-防御素是唯一已知的动物源性全环肽。由于所有六个θ-防御素假基因的信号序列中存在提前终止密码子，人类不产生θ-防御素肽。相反，由于推定的编码区的人θ-防御素假基因保持显着完整，其相应的肽，称为“retrocyclins”，已重建使用固相合成方法。作为HIV-1进入的抑制剂和杀菌剂，逆转录细胞周期蛋白表现出优异的治疗指数，这使得逆转录细胞周期蛋白成为进一步开发作为局部杀微生物剂以预防性传播疾病的有希望的候选物。本文综述了逆转录病毒的作用机制、逆转录病毒抑制剂在预防HIV-1性传播中的临床应用。
Primate theta-defensins are physically distinguished as the only known fully-cyclic peptides of animal origin. Humans do not produce theta-defensin peptides due to a premature stop codon present in the signal sequence of all six theta-defensin pseudogenes. Instead, since the putative coding regions of human theta-defensin pseudogenes have remained remarkably intact, their corresponding peptides, called “retrocyclins”, have been recreated using solid-phase synthetic approaches. Retrocyclins exhibit an exceptional therapeutic index both as inhibitors of HIV-1 entry and as bactericidal agents, which makes retrocyclins promising candidates for further development as topical microbicides to prevent sexually transmitted diseases. This review presents the evolution, antiretroviral mechanism of action, and potential clinical applications of retrocyclins to prevent sexual transmission of HIV-1.