Rational design of LEDGINs as first allosteric integrase inhibitors for the treatment of HIV infection.
Rational design of LEDGINs as first allosteric integrase inhibitors for the treatment of HIV infection.
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DOI：
10.1016/j.ddtec.2012.10.002
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发表时间：
2013-12-01
期刊：
影响因子：
--
通讯作者：
Debyser, Zeger
中科院分区：
文献类型：
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作者：
Desimmie, Belete A;Demeulemeester, Jonas;Debyser, Zeger
透镜上皮衍生生长因子（LEDGF/p75）和HIV-1整合酶（IN）之间的相互作用是抗病毒开发的有吸引力的靶点，因为其抑制阻断HIV复制。开发破坏LEDGF/p75-IN相互作用的新型小分子构成了治疗HIV的有希望的新治疗策略。在这里，我们将突出的小分子抑制剂的设计和开发结合的LEDGF/p75结合口袋的IN，称为LEDGIN的最新进展。
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.