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Ciapavir (SBI-0953294, cIAP1 antagonist for viral reactivation) is a bivalent, next-generation, Smac mimetic and antagonist of cIAP1 as latency-reversing agent (LRA), specifically and potently promote HIV-1 latency reversal activity both in vivo.Ciapavir's latency reversal activity is dependent on the NIK-dependent NF-κB signaling.Ciapavir exhibits substantially greater potency and efficacy as an LRA, inducing comparable levels of latency reversal at concentrations 10- to 1,000-fold lower than the first-generation molecule SBI-0637142, without an increase in cytotoxicity.Ciapavir does not trigger cytokine release or T cell activation.Ciapavir is capable of increasing latent HIV-1 expression in ART-treated BLT mice in vivo and may therefore prove useful in "shock and kill" approaches to HIV-1 cure.
Q308 is a small molecule that silences the latent HIV-1 provirus by inhibiting Tat-mediated gene transcription and selectively downregulates the expression levels of the facilitated chromatin transcription (FACT) complex.Q308 induced the preferential apoptosis in HIV-1 latently infected cells, Q308 may reduce the size of the viral reservoir.
GPS491 (EC50 = 0.47 μM) suppresses expression of the HIV-1 structural protein Gag and alters HIV-1 RNA accumulation, decreasing the abundance of RNAs encoding the structural proteins while increasing levels of viral RNAs encoding the regulatory proteins.
Emivirine is a non-nucleoside reverse transcriptase inhibitors (NNRTIs) that displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity.
Cyclotriazadisulfonamide (CADA) is a specific CD4-targeted HIV entry inhibitors. Cyclotriazadisulfonamide (CADA) inhibits the co-translational translocation of human CD4 (huCD4) into the ER lumen in a signal peptide (SP)-dependent way.
BRD-K98645985 is a class of 12-membered macrolactam and a BAF transcriptional repression inhibitor with an EC50 of ~2.37 µM. BRD-K98645985 binds ARID1A-specific BAF complexes, prevents nucleosomal positioning, and potently reverses HIV-1 latency, and without T cell activation or toxicity.
Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.
Nelfinavir(AG-1341) is a potent and orally bioavailable human immunodeficiency virus HIV-1 protease inhibitor (Ki=2 nM) and is widely prescribed in combination with HIV reverse transcriptase inhibitors for the treatment of HIV infection.
NBD-556 is small molecule mimetic of CD4, NBD-556 recognizes the HIV-1 envelope protein gp120 and induces restructuring of gp120 analogous to CD4 binding.
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