Reverse Transcriptase

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.

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.

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.

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.

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.

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.

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

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.

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

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.

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

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.

Telbivudine (NV 02B) is a Hepatitis B Virus Nucleoside Analog Reverse Transcriptase Inhibitor. The mechanism of action of telbivudine is as a Nucleoside Reverse Transcriptase Inhibitor. The chemical classification of telbivudine is Nucleoside Analog.

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 (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.

Tenofovir hydrate (GS 1278 hydrate) is a nucleotide reverse transcriptase inhibitor with antiviral activity, inhibits EBV replication, and is used in the study of HIV and HBV.

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).

Efavirenz (DMP 266) is a Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor, acting as a Non-Nucleoside Reverse Transcriptase Inhibitor, Cytochrome P450 3A Inducer, Cytochrome P450 2B6 Inducer, Cytochrome P450 2C9 Inhibitor, Cytochrome P450 2C19 Inhibitor, and Cytochrome P450 3A4 Inhibitor, classified as a Non-Nucleoside Analog.

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

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.

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.

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