Integrase plays a critical role in the recombination of viral DNA into the host genome. Therefore, over the past decade, it has been a hot target of drug design in the fight against type 1 human immunodeficiency virus (HIV-1). Bovine immunodeficiency virus (BIV) integrase has the same function as HIV-1 integrase. We have determined crystal structures of the BIV integrase catalytic core domain (CCD) in two different crystal forms at a resolution of 2.45 Å and 2.2 Å, respectively. In crystal form I, BIV integrase CCD forms a back-to-back dimer, in which the two active sites are on opposite sides. This has also been seen in many of the CCD structures of HIV-1 integrase that were determined previously. However, in crystal form II, BIV integrase CCD forms a novel face-to-face dimer in which the two active sites are close to each other. Strikingly, the distance separating the two active sites is approximately 20 Å, a distance that perfectly matches a 5-base pair interval. Based on these data, we propose a model for the interaction of integrase with its target DNA, which is also supported by many published biochemical data. Our results provide important clues for designing new inhibitors against HIV-1.

译文

:整合酶在病毒DNA重组入宿主基因组中起关键作用。因此,在过去的十年中,它已成为对抗1型人类免疫缺陷病毒(HIV-1)的药物设计的热门目标。牛免疫缺陷病毒(BIV)整合酶具有与HIV-1整合酶相同的功能。我们已经确定了BIV整合酶核心结构域(CCD)的晶体结构,其两种晶体形式的分辨率分别为2.45Å和2.2Å。在晶型I中,BIV集成CCD形成了一个背靠背的二聚体,其中两个活性位点在相反的一侧。在先前确定的HIV-1整合酶的许多CCD结构中也可以看到这一点。然而,在晶型II中,BIV集成CCD形成了一个新颖的面对面二聚体,其中两个活性位点彼此靠近。令人惊讶的是,两个有效位点之间的距离约为20,该距离与5个碱基对的间隔完全匹配。基于这些数据,我们提出了整合酶与其靶DNA相互作用的模型,许多已公开的生化数据也支持该模型。我们的结果为设计新的抗HIV-1抑制剂提供了重要线索。

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