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NNRTIs

Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV). NNRTIs inhibit reverse transcriptase (RT), anenzyme that controls the replication of the genetic material of HIV. RT is one of the most popular targets in the field of antiretroviral drug development. Drug resistance develops quickly if NNRTIs are administered as monotherapy and therefore NNRTIs are always given as part of combination therapy, the highly active antiretroviral therapy. The NNRTIs act by binding non-competitively to the RT enzyme. The binding causes conformational change in the three-dimensional structure of the enzyme and creates the NNIBP. Binding of NNRTI to HIV-1 RT makes the p66 thumb domain hyper extended because it induces rotamer conformation changes in amino acid residues Tyr-181 and Tyr-188. This affects the catalytic activity of the enzyme and blocks the HIV-1 replication by inhibiting the polymerase active site of the RT's p66 subunit.

Non-nucleoside reverse transcriptase inhibitors (9)
产品名称 目录号 简述
Dapivirine HY-14266

Dapivirine(TMC 120, TMC 120 R147681)是HIV非核苷逆转录酶抑制剂(NNRTI),IC50为24 nM,能抑制包括NNRTI抗性的各种HIV-1毒株。

Delavirdine HY-10571

Delavirdine(U 90152)是非核苷类逆转录酶抑制剂(NNRTI)。

Delavirdine mesylate HY-10571A

Delavirdine(U90152)甲磺酸盐是非核苷类逆转录酶抑制剂(NNRTI)。

Efavirenz HY-10572

Efavirenz (依非韦伦) 是非核苷类逆转录酶抑制剂(NNRTI),对野生型HIV-1 RT的Ki为2.93 nM。

Etravirine HY-90005

Etravirine (依曲韦林; R165335; TMC125)是非核苷类逆转录酶抑制剂,对野生型HIV-1的EC50为1.4 nM到4.8 nM。

Etravirine D4 HY-90005S

Etravirine D4是Etravirine氘代化合物标准品。

Lersivirine HY-14267

Lersivirine(UK-453061)是非核苷逆转录酶抑制剂(NNRTI),IC50为119 nM,对野生型和NNRTI抗性型毒株都有效。

Nevirapine HY-10570

Nevirapine (奈韦拉平) 是非核苷类逆转录酶抑制剂(NNRTI),可与核苷类似物结合用于抗HIV。

Rilpivirine HY-10574

Rilpivirine (利匹韦林; R278474, TMC 278) 是HIV的非核苷逆转录酶抑制剂。

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