合理设计LEDGINs作为首个用于治疗HIV感染的变构整合酶抑制剂。
Rational design of LEDGINs as first allosteric integrase inhibitors for the treatment of HIV infection.
作者信息
Desimmie Belete A, Demeulemeester Jonas, Christ Frauke, Debyser Zeger
出版信息
Drug Discov Today Technol. 2013 Dec;10(4):e517-22. doi: 10.1016/j.ddtec.2012.10.002.
The interaction between lens epithelium-derived growth factor (LEDGF/p75) and HIV-1 integrase (IN) is an attractive target for antiviral development because its inhibition blocks HIV replication. Developing novel small molecules that disrupt the LEDGF/p75-IN interaction constitutes a promising new therapeutic strategy for the treatment of HIV. Here we will highlight recent advances in the design and development of small-molecule inhibitors binding to the LEDGF/p75 binding pocket of IN, referred to as LEDGINs.
晶状体上皮衍生生长因子（LEDGF/p75）与HIV-1整合酶（IN）之间的相互作用是抗病毒研发的一个有吸引力的靶点，因为对其抑制可阻断HIV复制。开发能够破坏LEDGF/p75-IN相互作用的新型小分子构成了一种有前景的治疗HIV的新策略。在此，我们将重点介绍与IN的LEDGF/p75结合口袋结合的小分子抑制剂（称为LEDGINs）在设计和开发方面的最新进展。
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