reverse transcriptase

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.

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

1. Hypericin (Cyclosan) has antineoplastic activity. 2. Hypericin has antibiotic and antiviral activities. 3. Hypericin has antidepressive activity through inhibiting monoamine oxidase enzyme. 4. Hypericin inhibits RANKL-mediated osteoclastogenesis via affecting ERK signalling in vitro and suppresses wear particle-induced osteolysis in vivo.

Tenofovir (GS 1278) is an adenine analog REVERSE TRANSC-RIPTASE INHIBITOR with antiviral activity against HIV-1 and HEPATITIS B. It is used to treat HIV INFECTIONS and CHRONIC HEPATITIS B, in combination with other ANTIVIRAL AGENTS, due to the emergence of ANTIVIRAL DRUG RESISTANCE when it is used alone.

Emtricitabine (FTC) (FTC), a nucleoside reverse transcriptase inhibitor, exhibits inhibition activity against human immunodeficiency virus (HIV) and hepatitis B virus.

Gramine (Donaxine), a natural indole alkaloid, present in several plant species, acts as an active adiponectin receptor (AdipoR) agonist, with IC50s of 3.2 and 4.2 μM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist. Gramine has anti-tumor, anti-viral and anti-inflammatory properties.

Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.

Tenofovir Disoproxil Fumarate (GS-1278 Disoproxil Fumarate) is a pro-drug, fumaric acid salt form of tenofovir, a nucleoside reverse transcriptase inhibitor analog of adenosine. Tenofovir disoproxil fumarate is prescribed to treat HIV and chronic hepatitis B virus (HBV) in adults.

Tenofovir alafenamide (GS-7340) is a nucleotide reverse transcriptase inhibitor (NRTI) and a novel ester prodrug of the antiretroviral tenofovir.

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.

(Iso)-Fosdevirine ( (Iso)-GSK2248761) is a selective and potent non-nucleoside reverse transcriptase (NNRTI) inhibitor with anti-HIV activity for the study of neurological disorders such as late-onset epilepsy.

KM-023 is a new second-generation non-nucleoside reverse transcriptase inhibitor for the study of human immunodeficiency virus (HIV) type 1 infection.

IQP-0528 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) that has potential for the treatment of HIV infection by blocking viral entry and shows antiviral activity as a microbicidal gel. . IQP-0528 showed inhibition of both HIV-1 and HIV-2, with an EC50 of 0.2 nM for HIV-1 and 100 nM for HIV-2.

Metacavir (PNA) is a novel nucleoside reverse transcriptase inhibitor, a deoxyguanosine analog, with anti-hepatitis B virus (HBV) activity and mitochondrial toxicity, which can be used to study HBV infection.

MK-6186 HCl, a novel non-nucleoside reverse transcriptase inhibitor with antiviral activity, can be used to study HIV.

Opaviraline (GW-420867X) is a potent reverse transcriptase inhibitor that inhibits Human immunodeficiency virus 1 and has the potential to treat HIV infection.

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.

Fosdevirine (GSK2248761) is a selective and potent non-nucleoside reverse transcriptase (NNRTI) inhibitor with anti-HIV activity for the study of neurological related disorders such as late-onset epilepsy.

Netivudine is a potent nucleoside reverse transcriptase inhibitor (NRTIs), a nucleoside analogue with anti-varicella zoster virus activity that can be used to treat human immunodeficiency virus (HIV) infection. Netivudine works by inhibiting reverse transcriptase, which reduces viral load in the body and slows the progression of the disease through its inhibitory effect.

(R,1R)-Tenofovir amibufenamide ((R,1R)-HS-10234) can be used as a Tenofovir prodrug, which can be taken orally and has antiviral activity. Tynofovir is a nucleotide reverse transcriptase inhibitor.

BF738735 is a selective inhibitor of phosphatidylinositol 4-kinase III beta (PI4KIIIβ, IC50 = 5.7 nM) showing higher activity over α(IC50 = 1.7 μM). BF738735 exhibits a broad spectrum of antiviral activity.

AzddMeC (Az-Dcme) is a nucleoside analog with antiviral activity and is an orally active and selective inhibitor of HIV-1 reverse transcriptase and HIV-1 replication.AzddMeC has an EC50 value of 9 nM against HIV-1-infected human PBM cells and 6 nM against HIV-1-infected human macrophages.

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.

Adefovir dipivoxil (GS 0840) is a dipivoxil formulation of adefovir, a nucleoside reverse transcriptase inhibitor analog of adenosine with activity against hepatitis B virus (HBV), herpes virus, and human immunodeficiency virus (HIV).

Etravirine (R165335) is a diarylpyrimidine non-nucleoside reverse transcriptase inhibitor. Etravirine is designed to be active against HIV isolates with mutations that confer resistance to the two most commonly prescribed first-generation NNRTIs. It can bind the enzyme reverse transcriptase (RT) in multiple conformations, both for native and mutant RT, thereby blocking the enzymatic activity of RT.

Abacavir (Ziagen) is a nucleoside reverse transcriptase inhibitor analog of guanosine. This agent decreases HIV viral loads, retards or prevents the damage to the immune system, and reduces the risk of developing AIDS.

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.

Tenofovir Disoproxil (GS 4331) is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.

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.

Dapivirine (R147681) is a diarylpyrimidine non-nucleoside reverse transcriptase inhibitor.

Efavirenz (DMP 266) is a Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor. The mechanism of action of efavirenz is as a Non-Nucleoside Reverse Transcriptase Inhibitor, and Cytochrome P450 3A Inducer, and Cytochrome P450 2B6 Inducer, and Cytochrome P450 2C9 Inhibitor, and Cytochrome P450 2C19 Inhibitor, and Cytochrome P450 3A4 Inhibitor. The chemical classification of efavirenz is Non-Nucleoside Analog.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Didanosine (ddI) is a nucleoside reverse transcriptase inhibitor analog of adenosine (IC50: 0.49 μM).

Tizoxanide (Desacetyl-nitazoxanide) is a metabolite of lamivudine. Lamivudine (2', 3'-dideoxy-3'-thiacytidine, commonly called 3TC) is a potent nucleoside analog reverse transcriptase inhibitor (nRTI).

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

Methyl gallate (Gallincin) is a reverse transcriptase inhibitor with antioxidant, anti-HIV-1 and HIV-1 enzyme inhibition activities.

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).

Daidzin (Daidzoside) is an isoflavone isolated from soya bean with anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities.

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

Suramin is a reversible, competitive inhibitor of protein-tyrosine phosphatases (PTPases) [1], demonstrating potent inhibition against sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) [2]. It also acts as a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) [3] [4] and exhibits potent inhibition of SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) [5]. Additionally, Suramin effectively inhibits IP5K, showcasing its antiparasitic, anti-neoplastic, and anti-angiogenic properties [6] [7] [8].

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.

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].

Liquidambaric lactone is a compound isolated from Euonymus grandiflorus Wall.Liquidambaric lactone may have inhibitory HIV-1 reverse transcriptase activity.

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

Delavirdine is a non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine is part of Highly Active Antiretroviral Therapy (HAART), which can be used to treat human immunodeficiency virus (HIV) type 1.

Lamivudine 13C,15N2, an impurity of Lamivudine (BCH-189), functions as an inhibitor of both HIV-1/2 reverse transcriptase and hepatitis B virus reverse transcriptase, classifying it as a nucleoside reverse transcriptase inhibitor (NRTIs).

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.

Lersivirine (UK-453061)(UK 453061) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) under development for HIV infection therapy.

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).