tenofovir diphosphate

Tenofovir diphosphate is an inhibitor of HIV reverse transcriptase (Kis = 0.022 and 1.55 μM for RNA and DNA, respectively) and hepatitis B virus (HBV) polymerase (Ki = 0.18 μM). It is selective for these enzymes over DNA polymerase α and β, as well as mitochondrial DNA polymerase γ (Kis = 5.2, 81.7, and 59.5 μM, respectively). Tenofovir diphosphate is formed intracellularly through phosphorylation of the prodrugs tenofovir and tenofovir disoproxil by nucleotide kinases. Increased levels of tenofovir diphosphate in isolated peripheral blood mononuclear cells (PBMCs) correlate with a decrease in the risk of simian HIV (SHIV) acquisition in a macaque model of rectal SHIV transmission.

Tenofovir diphosphate (TFV-DP) is a competitive inhibitor of DNA polymerases, specifically targeting dATP, and it serves as a substrate for the reverse transcriptase (RT) of human immunodeficiency virus type 1 (HIV-1)[1].

Tenofovir diphosphate TEA （TFV-DP TEA）是TFV-DP的三乙胺盐，是一种ATP竞争性的DNA聚合酶 (DNA polymerases) 抑制剂，能够抑制HIV-1逆转录酶（HIV-1 reverse transcriptase）。它通过掺入病毒DNA链中，终止病毒DNA的合成，从而抑制病毒基因组的复制，具有抗HIV HBV的潜力。