Reverse Transcriptase

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.

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.

Bifendate (Bifendatatum) is commonly used to treat the transaminase elevation that caused by viral hepatitis and drug-induced liver injury.

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.

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

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

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.

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).

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.

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.

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

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.

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

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

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.

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.

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

Zidovudine (ZDV) is a synthetic dideoxynucleoside. After intracellular phosphorylation to its active metabolite, zidovudine inhibits DNA polymerase, resulting in the inhibition of DNA replication and cell death. This agent also decreases levels of available pyrimidines.

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

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).

Alizarin Complexone (Alizarin-3-methyliminodiacetic acid) is an inhibitor of Rous-associated virus 2 reverse transcriptase. Alizarin Complexone can be used as a calcium-tracer and a chelating agent for biological studies.

ddUTP (2′,3′-Dideoxyuridine-5′-triphosphate) serves as a selective inhibitor of HIV and AMV reverse transcriptases with Ki values of 0.05 µM for HIV and 1 µM for AMV, respectively. This compound is preferentially incorporated at dTTP sites within the DNA strand, thereby preventing further chain elongation [1].

R-10015 is a highly potent and selective LIMK inhibitor that blocks LIMK by binding to the ATP-binding pocket. It inhibits human LIMK1 with an IC50 value of 38 nM. It also exerts broad-spectrum antiviral effects and may be used in HIV infection research.

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

2,2'-Anhydrouridine (2,2'-Cyclouridine) is a research tool for antiviral and anticancer studies.

Emtricitabine, a potent nucleoside reverse transcriptase inhibitor, is employed for managing HIV infection. Emtricitabine S-oxide, also known as Emtricitabine sulfoxide, represents a significant degradation byproduct of Emtricitabine.

Emtricitabine triphosphate tetrasodium salt is the tetrasodium salt form of the phosphorylated anabolite (-)-Emtricitabine triphosphate, an active nucleoside reverse transcriptase inhibitor that is effective against HIV and HBV [1].

Salicylanilide (2-Hydroxybenzanilide)s are a group of compounds with antiviral potency, antibacterial and antifungal activities.

Foscarnet sodium (Phosphonoformate) is an antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.

Pyridoxal phosphate (Vitamin B6 phosphate) is the active form of vitamin B6 and a coenzyme for many pyridoxal phosphate (PLP)-dependent enzymes. PLP is involved in numerous enzymatic transamination, decarboxylation and deamination reactions; it is necessary for the synthesis of amino acids and amino acid metabolites, and for the synthesis and or catabolism of certain neurotransmitters, including the conversion of glutamate into gamma-aminobutyric acid (GABA) and levodopa into dopamine. PLP can be used as a dietary supplement in cases of vitamin B6 deficiency. Reduced levels of PLP in the brain can cause neurological dysfunction.

MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with antiviral activity for the study of viral infections.

EFdA-TP tetrasodium, a potent nucleoside reverse transcriptase (RT) inhibitor, effectively halts RT-catalyzed DNA synthesis by acting as an immediate or delayed chain terminator (ICT or DCT). It employs multiple mechanisms to inhibit HIV-1 RT [1].

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

Zalcitabine (Dideoxycytidine)(Dideoxycytidine;ddC; 2', 3'-Dideoxycytidine) is a nucleoside analog reverse transcriptase inhibitor (NRTI); At low concentrations, It can potently inhibit HIV replication by binding to reverse transcriptase terminated synthesis of viral DNA chain.

AG 555 (Tyrphostin B46) is an EGFR tyrosine kinase inhibitor.

RO-0335 is a potent diphenylether nonnucleoside reverse transcriptase inhibitor. RO-0335 inhibits Wt HIV-1 (IC50 = 1.1 nM) and retained activity (IC50< 100 nM) against 92% of a large number of NNRTI-resistant clinical isolates.

Dexelvucitabine (RVT), a nucleoside reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.

Censavudine (OBP-601) is a nucleoside analog, a nucleoside reverse transcriptase inhibitor, used for the prevention and treatment of human immunodeficiency virus 1 (HIV-1).Censavudine inhibits HIV-2 and HIV-1. Censavudine inhibits HIV-2 and HIV-1 with EC50 ranges of 30-81 nM and 450-890 nM, respectively.

Abacavir sulfate (Ziagen) , a nucleoside analogue, effectively utilize its antiviral activity

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

Corilagin has anti-inflammatory activity. Corilagin has a significant antitumour potential and lower toxicity in normal cells in vitro.Corilagin can enhance the cytotoxicity of both cisplatin and doxorubicin on the Hep3B hepatoma cells.Corilagin has antiviral activity, reduces the cytotoxicity induced by EV71 or CA16 on Vero cells with and IC50 value of 5.6 and 32.33 μg/mL, respectively. Corilagin shows the potential to protect against HSV-1-induced encephalitis, and the beneficial effects may be mediated by inhibiting TLR2 signaling pathways.Corilagin has antifibrotics property and is potentiated in treating idiopathic pulmonary fibrosis(IPF), attenuates bleomycin-induced epithelial injury and fibrosis via inactivation of oxidative stress, proinflammatory cytokine release and NF-κB and TGF-β1 signaling. Solvent:Pyridine, Methanol, Ethanol, etc.

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an oral phosphonoamidate prodrug of the HIV reverse transcriptase nucleotide inhibitor tenofovir (TFV)

Islatravir (MK-8591) is an effective anti-HIV-1 agent. It acts as a nucleoside reverse transcriptase inhibitor (EC50s: 0.068 nM, 3.1 nM, and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively).

Adefovir is an acyclic nucleoside phosphonate that acts as a reverse transcriptase inhibitor used for treatment of hepatitis B and herpes simplex virus infection.

Azvudine (FNC) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine inhibits NRTI-resistant viral strains. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM).