Anatomy and pathology of HIV-1 peptidase.
Anatomy and pathology of HIV-1 peptidase.
复制标题
HIV-1 肽酶的解剖学和病理学。
DOI：
10.1042/bse0380113
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发表时间：
2002
影响因子：
6.4
通讯作者：
Dunn,BenM
中科院分区：
文献类型：
--
作者：
Dunn,BenM
HIV 1型（HIV PR）的肽酶是病毒复制和进一步感染所必需的。在过去的15年里，人们共同努力了解这种酶的特性，因为它是控制病毒的一个很好的药物靶点。由于药物压力，在病毒周转期间出现许多突变，其中一些突变导致对抑制剂作用的耐药性。这些突变导致的酶的变化及其与底物和抑制剂的相互作用的理解的最新进展已被描述。此外，对来自猿免疫缺陷病毒、猫免疫缺陷病毒和HIV-2的密切相关的逆转录病毒酶的研究扩大了结构-功能范例。的灵活性的配体和活性位点相互作用的酶的作用进行了讨论。
The peptidase of the HIV type 1 (HIV PR) is required for the replication of and further infection by the virus. A concerted effort has taken place in the past 15 years to understand the properties of this enzyme, as it serves as an excellent drug target for control of the virus. Owing to drug pressure, many mutations arise during turnover of the virus and some of these lead to resistance to the effects of the inhibitors. Recent advances in the understanding of the changes these mutations cause to the enzyme and its interaction with substrates and inhibitors have been described. In addition, studies of closely related retroviral enzymes from simian immunodeficiency virus, feline immunodeficiency virus and HIV-2 have expanded the structure-function paradigm. The role of the flexibility of ligands and of the enzyme in active-site interactions is discussed.