Signaling Pathway

NNRTIs

NNRTIs

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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.

NNRTIs Inhibitors & Modulators (9)

Product Name Catalog No. Brief Description
Dapivirine

HY-14266

Dapivirine(TMC 120, TMC 120 R147681) is a NNRTI for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates.

Delavirdine

HY-10571

Delavirdine(U 90152) is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI).

Delavirdine mesylate

HY-10571A

Delavirdine(U 90152) mesylate is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI).

Efavirenz

HY-10572

Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI).

Etravirine

HY-90005

Etravirine (R165335; TMC125) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.

Etravirine D4

HY-90005S

Etravirine D4 is the deuterium labeled Etravirine, which is a NNRTI  used for the treatment of HIV.

Lersivirine

HY-14267

Lersivirine(UK-453061) is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI, IC50=119 nM) with a unique resistance profile that exhibits potent antiretroviral activity against wild-type human immunodeficiency virus and clinically relevant NNRTI-resistant strains.

Nevirapine

HY-10570

Nevirapine is a potent, non-nucleoside reverse transcriptase inhibitor (NNRTI) used in combination with nucleoside analogues for treatment of HIV-1 infection and AIDS.

Rilpivirine

HY-10574

Rilpivirine(R 278474, TMC 278) is a type of anti-HIV medicine called a non-nucleoside reverse transcriptase inhibitor (NNRTI).