Desimmie Belete A, Demeulemeester Jonas, Christ Frauke, Debyser Zeger
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。
