reverse transcriptase in 1

Reverse transcriptase-IN-1 is a diarylbenzopyrimidine (DABP) analogue and a potent inhibitor of HIV-1 nonnucleoside reverse transcriptase with an IC50of 13.7 nM.

Reverse transcriptase-IN-4 is a potent, selective non-nucleoside reverse transcriptase (NNRT) inhibitor, demonstrating an EC50 of 0.053 μM against wild-type HIV-1 and 0.26 μM for the E138K HIV-1 mutant.

Reverse transcriptase-IN-3, a pyrimidine-5-carboxamide derivative, functions as an inhibitor of HIV-1, demonstrating potent activity against both wild-type and mutant strains of HIV-1.

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.

Nevirapine (NVP) is a benzodiazepine non-nucleoside reverse transcriptase inhibitor. In combination with other antiretroviral drugs, nevirapine reduces HIV viral loads and increases CD4 counts, thereby retarding or preventing the damage to the immune system and reducing the risk of developing AIDS.

Lamivudine (BCH-189) is a reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.

UC-781 (NSC-675186) is a potent and selective inhibitor of human immunodeficiency virus HIV-1 non-nucleoside reverse transcriptase (NNRTI) I with a C50 value of 5 nM.UC-781 exhibits both antiviral activity and drug resistance.UC-781 is in a stable state, and is unaffected by lower pH or varying temperatures.

Rilpivirine (R278474) is a diarylpyrimidine derivative and reverse transcriptase inhibitor with antiviral activity against HIV-1 that is used in the treatment of HIV infections.

Doravirine (MK-1439) is a non-nucleoside reverse transcriptase inhibitor used for the treatment of HIV AIDS.

Punicalin exerts anti-inflammatory, antioxidative, and anti-hepatotoxic activities, it shows inhibitory activity on HIV-1 reverse transcriptase in a dose-dependent manner, with an IC50 of 0.11 microg ml (0.14 microM).

EFdA-TP, a highly potent nucleoside reverse transcriptase (RT) inhibitor, exerts its inhibitory effect on RT-catalyzed DNA synthesis through both immediate and delayed chain termination mechanisms, commonly referred to as ICT and DCT, respectively. Additionally, EFdA-TP demonstrates its efficacy in inhibiting HIV-1 RT through multiple pathways.

AIC-292 is a potent reverse transcriptase inhibitor with well tolerated in different cell lines. In addition, activity of AIC292 could be demonstrated against a broad panel of wild-type HIV-1 group. AIC292 also retained activity against viruses harboring

Pol (476-484), HIV-1 RT Epitope, is a biologically active peptide representing the dominant HLA A*0201-restricted epitope within HIV-1 reverse transcriptase (RT). Spanning Pol residues 476-484, it is utilized to explore mechanisms of HIV-1 escape from cytotoxic T lymphocytes (CTL) with IV9 as the specific epitope processed and presented in HIV-1-infected cell lines.

HIV-1 Inhibitor-49, a HEPT analog, is an orally active non-nucleoside reverse transcriptase inhibitor with potent activity against HIV-1, demonstrating an IC 50 of 30 nM. It features an excellent pharmacokinetic profile and has shown to be potentially safe without acute toxicity in mouse models.

HIV-1 Inhibitor-61 (2c) serves as a potent inhibitor of HIV-1 reverse transcriptase, exhibiting an EC50 value of 0.07 nM in NL4-3 wt MT-4 cells [1].

Abacavir monosulfate is an orally active, competitive nucleoside reverse transcriptase inhibitor that effectively inhibits HIV replication. Additionally, it exhibits anticancer properties in prostate cancer cell lines, and has the ability to penetrate the blood-brain-barrier and suppress telomerase activity [1] [2] [3].

SM111 inhibits in vitro replication of HIV-1, including strains resistant to reverse transcriptase, licensed protease, and integrase inhibitors, without major cellular toxicity.

(+)-Carbovir triphosphate, an active metabolite of Abacavir, was utilized to study the molecular mechanism of inhibition and drug resistance in HIV-1 reverse transcriptase.

HIV-1 Inhibitor-57 (Compound 12g) is an antiviral agent that potently inhibits both wild-type and five common NNRTI-resistant strains of HIV-1, exhibiting EC50 values between 0.024 and 0.0010 μM. It achieves this efficacy by forming supplementary interactions with residues surrounding the binding site in the HIV-1 reverse transcriptase (RT) [1].

Murabutide, a safe synthetic immunomodulator, diminishes the expression of CD4 and CCR5 receptors and promotes the secretion of high levels of beta-chemokines, thereby enhancing nonspecific resistance to viral infections. It does not impact virus entry, reverse transcriptase activity, or the formation of early proviral DNA in the cytoplasm of infected cells [1].

beta-L-D4A, a nucleoside HIV-1 reverse transcriptase inhibitor, exhibits biological activity by terminating DNA chain synthesis in the 5'-3' direction.

Loviride is a non-nucleoside reverse transcriptase inhibitor (IC50: 0.3 µM). Loviride inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells. It is used for reverse transcriptase from HIV-1.

HIV-1 inhibitor-23 is a highly potent inhibitor of HIV-1 non-nucleoside reverse transcriptase, acting on both wild-type HIV-1 (EC50: 24.9 nM) and mutant strain K103N (EC50: 10.4 nM). microsomal stability in vitro.

ZLM-66 is a doravirine analogue and a potent inhibitor of non-nucleoside reverse transcriptases (NNRTIs), acting on wild-type HIV-1 reverse transcriptase (IC50: 41 nM), wild-type HIV-1 (EC50: 13 nM) and cIAP1 (EC50: 0.32 nM). ZLM-66 can be used in AIDS research.

NNRT-IN-2 (compound 7w) is an orally administered non-nucleoside reverse transcriptase inhibitor (NNRTI) that effectively suppresses both wild-type HIV-1 and various mutant strains. It inhibits HIV-1 reverse transcriptase with an EC 50 value of 22 nM. Additionally, NNRT-IN-2 exhibits insensitivity to CYP and hERG, demonstrating favorable safety and pharmacokinetic profiles [1].

Hydroxyisoquinoline-1,3(2H,4H)-dione (compound 6a) acts as an inhibitor of both HIV-1 integrase (IN) and HIV-1 reverse transcriptase ribonuclease H (RT RNase H), exhibiting IC50 values of 6.32 µM and 5.9 µM, respectively.

Nevirapine-d3 is a deuterated compound of Nevirapine. Nevirapine has a CAS number of 129618-40-2. Nevirapine is a benzodiazepine non-nucleoside reverse transcriptase inhibitor. In combination with other antiretroviral drugs, nevirapine reduces HIV viral loads and increases CD4 counts, thereby retarding or preventing the damage to the immune system and reducing the risk of developing AIDS.

Lamivudine-13C-d2 the 13C and deuterated compound of Lamivudine. Lamivudine has a CAS number of 134678-17-4. Lamivudine is a reverse transcriptase inhibitor and ZALCITABINE analog in which a sulfur atom replaces the 3' carbon of the pentose ring. It is used to treat HIV disease.

HIV-1 Inhibitor-58 (Compound 10c) is a non-nucleoside reverse transcriptase inhibitor with broad-spectrum antiviral properties, effective against both wild-type strain IIIB and NNRTI-resistant strains like K103N and E138K in MT-4 cells at an EC50 of less than 50 nM. Additionally, it inhibits CYP2C9 and CYP2C19 with IC50 values of 2.06 μM and 1.91 μM, respectively. This compound is utilized in HIV infection research [1].

5,7,3',5'-tetrahydroxy-6,4'-dimethoxyflavone exhibits anti-HIV-1 activity in the anti-syncytium assay using (∆Tat/rev)MC99 virus and 1A2 cell line system, it shows considerably activity against HIV-1 reverse transcriptase. It exhibits cytotoxic activity against P-388 cell lines, it can inhibit DNA topoisomerase IIα activity, which may be responsible for the observed cytotoxicity.

INDOPY-1 is a Nucleotide-Competing Reverse Transcriptase Inhibitor. INDOPY-1 was the first NcRTI discovered, displaying reversible competitive inhibition of dNTP binding. 3,4 Biochemical studies showed that INDOPY-1 arrests RT/DNA in a post-translocated (P site) complex.

NNRTIs-IN-1 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) with notable anti-resistance efficacy, effectively inhibiting both the wild-type HIV-1 and five mutant strains at EC50 values within the nanomolar range. This compound also exhibits favorable pharmacokinetic properties [1].

HIV-1 inhibitor-56 (compound 12126065) is a potent non-nucleoside reverse transcriptase inhibitor with significant antiviral activity against wild-type HIV-1, exhibiting an EC50 value of 0.24 nM in TZM cells, and is capable of penetrating the blood-brain barrier [1].

R-82913 is a RNA-directed DNA polymerase inhibitor. R 82913 reduce 5-HT2 receptor-mediated DOI-head-shakes in mice. R82913 inhibited the replication of thirteen different strains of HIV-1 in CEM cells with a median IC50 of 0.15 microM. R82913 was 20-fold

HIV-IN-5 (compound 5r) is a potent inhibitor of HIV-1 with an IC50 of 0.16 μM, binding to NNIBP [NNRTIs (non-nucleoside reverse transcriptase inhibitors) binding sites].

Stampidine can prevent the sexual transmission of HIV-1. It exhibited remarkable subnanomolar to low nanomolar in vitro antiretroviral potency against nucleoside reverse transcriptase inhibitor-resistant primary clinical HIV isolates, non-nucleoside RT-re

Isoguanosine-5'-O-triphosphate, an isomer of guanosine 5'-triphosphate (GTP) and a phosphorylated derivative of crotonoside, does not promote microtubule assembly like GTP. At a concentration of 2 mM, it hampers transcription and triggers T to C mutations in reverse transcriptase assays. This compound aids in assessing the substrate specificity of both phosphofructokinase and mutT homolog 1 (MTH1).

HIV-1 inhibitor-46 (compound 13d) is a potent non-nucleoside reverse transcriptase inhibitor of HIV-1 with an EC50 of 1.425 μM. This compound is suitable for use in AIDS research.

Sp-Thymidine-5'-O-(1-thiotriphosphate) (Sp-TTP-α-S), an isomer of the sulfur-containing nucleotide derivative TTP-α-S, exhibits affinity for HIV-1 reverse transcriptase with dissociation constants (Kds) of 2.88, 4.23, and 20.21 µM in the presence of magnesium, manganate, and cobalt, respectively. Additionally, Sp-TTP-α-S effectively inhibits the enzyme deoxynucleoside triphosphate triphosphohydrolase SAMHD1 with an inhibition constant (Ki) of 46 nM.

Nevirapine-d4 is a deuterated compound of Nevirapine. Nevirapine has a CAS number of 129618-40-2. Nevirapine is a benzodiazepine non-nucleoside reverse transcriptase inhibitor. In combination with other antiretroviral drugs, nevirapine reduces HIV viral loads and increases CD4 counts, thereby retarding or preventing the damage to the immune system and reducing the risk of developing AIDS.

NNRTIs-IN-3 (compound 8) is an HIV-1 non-nucleoside reverse transcriptase inhibitor, displaying potent efficacy with an EC50 value of 0.01 µM [1].

β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group, but it was revised to a para-quinone group in 2000 using organic and biosynthetic methods, as well as spectroscopic analysis.1,2,3References1. Ueno, T., Takahashi, H., Oda, M., et al. Inhibition of human telomerase by rubromycins: Implication of spiroketal system of the compounds as an active moiety. Biochemistry 39(20), 5995-6002 (2000).2. Puder, C., Loya, S., Hizi, A., et al. Structural and biosynthetic investigations of the rubromycins. Eur. J. Org. Chem. 2000(5), 729-735 (2000).3. Goldman, M.E., Salituro, G.S., Bowen, J.A., et al. Inhibition of human immunodeficiency virus-1 reverse transcriptase activity by rubromycins: Competitive interaction at the template.primer site. Mol. Pharmacol. 38(1), 20-25 (1990). β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, respectively. β-rubromycin inhibits HIV-1 reverse transcriptase activity by 39.7% when used at a concentration of 10 μM. It also has antibacterial activity against Gram-positive bacteria. The structure of β-rubromycin was originally described as containing an ortho-quinone group, but it was revised to a para-quinone group in 2000 using organic and biosynthetic methods, as well as spectroscopic analysis.1,2,3 References1. Ueno, T., Takahashi, H., Oda, M., et al. Inhibition of human telomerase by rubromycins: Implication of spiroketal system of the compounds as an active moiety. Biochemistry 39(20), 5995-6002 (2000).2. Puder, C., Loya, S., Hizi, A., et al. Structural and biosynthetic investigations of the rubromycins. Eur. J. Org. Chem. 2000(5), 729-735 (2000).3. Goldman, M.E., Salituro, G.S., Bowen, J.A., et al. Inhibition of human immunodeficiency virus-1 reverse transcriptase activity by rubromycins: Competitive interaction at the template.primer site. Mol. Pharmacol. 38(1), 20-25 (1990).

HIV-1 inhibitor-40 (Compound 4ab), an HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) with an EC50 of 1.9 nM, exhibits no significant acute toxicity in vivo and functions as a highly sensitive inhibitor of the orexin receptor antagonist CYP.

L-696229 is a specific inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). L-696229 inhibited RT activity in a mutually exclusive manner with respect to either phosphonoformate or azidothymidine triphosphate and was a weak

Vitexilactone is a HIV-1 reverse transcriptase inhibitor in virtual screening against Indonesian Herbal Database using AutoDock4 performed on HIV-1 reverse transcriptase. It has trypanocidal activity, the minimum lethal concentration against epimastigotes

Inophyllum B ((+)-Inophyllum B), a compound extracted from the acetone extract of the giant African snail, Achatina fulica [1], serves as a potent inhibitor of HIV Reverse Transcriptase with an IC50 value of 38 nM and exhibits inhibitory effects against HIV-1 in vitro cell culture with an IC50 of 1.4 μM.

4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, demonstrates potent activity against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity.

GSK 224876 is a novel next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI). It has activity against efavirenz-resistant strains in the treatment of treatment-naive HIV-1-infected subjects.