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Evolving understanding of HIV-1 reverse transcriptase structure, function, inhibition, and resistance.
Current Opinion in Structural Biology ( IF 6.8 ) Pub Date : 2020-01-11 , DOI: 10.1016/j.sbi.2019.11.011
Francesc Xavier Ruiz 1 , Eddy Arnold 1
Affiliation  

The essential role of reverse transcription in the HIV life cycle is illustrated by the fact that half of the ∼30 FDA-approved drugs for HIV treatment target HIV-1 reverse transcriptase (RT). Even though more than 160 structures of RT deposited in the Protein Data Bank (PDB) have revealed the molecular architecture of RT in great detail, some key states of RT function and inhibition remain still unknown. Recent structures of RT initiation complexes, RT poised for RNA hydrolysis, and RT with approved drugs and investigational compounds have provided a deeper understanding of RT function and inhibition, suggesting novel avenues for targeting this central enzyme of HIV.

中文翻译:

对HIV-1逆转录酶的结构,功能,抑制和抗性的不断发展的了解。

事实证明,在大约30种FDA批准的用于HIV治疗的药物中,有一半靶向HIV-1逆转录酶(RT),从而说明了逆转录在HIV生命周期中的重要作用。尽管蛋白质数据库(PDB)中沉积的RT结构超过160种,已详细揭示了RT的分子结构,但RT功能和抑制的一些关键状态仍然未知。RT起始复合物的最新结构,准备用于RNA水解的RT和具有批准的药物和研究性化合物的RT提供了对RT功能和抑制作用的更深刻理解,为靶向此HIV核心酶提供了新途径。
更新日期:2020-01-11
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