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Application of technologies and parallel chemistry for the generation of actives against biological targets

机译：技术和平行化学在产生针对生物靶标的活性剂中的应用

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The reverse transcriptase (RT) of H1V-1 is an essential enzyme in the lifecycle of the retro-virus. After entering the cell, RT copies the viral plus sense and single-stranded genomic RNA into double-stranded DNA. This process is catalyzed solely by RT and depends on two fundamental enzymatic activities: that of the DNA polymerase (which copies both RNA and DNA into DNA) and that of the RNaseH, which con-comitantly cleaves the viral RNA strand in the RNA/DNA heteroduplex. The resulting double-stranded DNA is transported into the nucleus as part of a pre-integration complex and is subsequently incorporated into the DNA of the cell by the viral enzyme integrase . An intense worldwide search for molecules that block RT activities is still in progress. To date, research efforts have led to several classes of inhibitors of HIV; one such class is the non-nucleoside RT inhibitors (NNRTIs). NNRTIs are a variety of noncompetitive inhibitors that bind specifically to a hydrophobic pocket in proximity to the DNA polymerase active site of the enzyme. The majority of inhibitors are highly specific against HIV-1 RT with minimal effects on the closely related HIV-2 RT . This class of inhibitor is used in therapy against HIV-1 as part of the highly active anti-retroviral therapy (HAART). A significant obstacle for the use of NNRTIs is their very high specificity that reduces their efficacy against mutated variants of the virus .
机译：H1V-1的逆转录酶（RT）是逆转录病毒生命周期中必不可少的酶。进入细胞后，RT将病毒加有义和单链基因组RNA复制为双链DNA。此过程仅由RT催化，并取决于两个基本的酶促活性：DNA聚合酶的活性（将RNA和DNA都复制到DNA中）和RNaseH的活性，其同时裂解RNA / DNA中的病毒RNA链。异源双工。所得的双链DNA作为预整合复合物的一部分转运到细胞核中，随后通过病毒酶整合酶整合到细胞的DNA中。仍在全球范围内对阻止RT活动的分子进行深入研究。迄今为止，研究工作已经导致了几类HIV抑制剂。一种这样的类别是非核苷RT抑制剂（NNRTI）。 NNRTIs是多种非竞争性抑制剂，可特异性结合至靠近酶DNA聚合酶活性位点的疏水口袋。大多数抑制剂对HIV-1 RT具有高度特异性，而对密切相关的HIV-2 RT影响最小。这类抑制剂被用作抗HIV-1的疗法，是高活性抗逆转录病毒疗法（HAART）的一部分。使用NNRTIs的一个重要障碍是其很高的特异性，降低了它们对病毒突变变异体的效力。

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