Edoxudine (EUDR)

Edoxudine (EUDR) is a deoxy-thymidine analog shown to be effective against herpes simplex virus type 1 and type 2 ^[1]. Edoxudine has been shown in vertebrate systems to be phosphorylated preferentially by the thymidine kinase and incorporated into viral DNA, and inhibiting viral DNA synthesis^[2]. Edoxudine disrupts the outer wall of Klebsiella pneumoniae and damages the protective effect of the LPS layer, making the cell membrane of Klebsiella pneumoniae accessible to antibacterial effectors^[3]. Edoxudine has been widely used as a lead compound for the development of drugs targeting the surface protein of monkeypox virus E8 ^[4].

In vitro, Edoxudine treatment for 72 hours significantly inhibited the proliferation of human foreskin fibroblasts (HFFs), with an IC₅₀ value of 115µM^[5].

References:
[1] Sharma A, Tiwari V, Sowdhamini R. Computational search for potential COVID-19 drugs from FDA-approved drugs and small molecules of natural origin identifies several anti-virals and plant products[J]. Journal of biosciences, 2020, 45(1): 100.
[2] Mazzacano C A, Fallon A M. Evaluation of a viral thymidine kinase gene for suicide selection in transfected mosquito cells[J]. Insect molecular biology, 1995, 4(2): 125-134.
[3] Ifrid E, Ouertatani-Sakouhi H, Jauslin T, et al. 5-ethyl-2’-deoxyuridine fragilizes Klebsiella pneumoniae outer wall and facilitates intracellular killing by phagocytic cells[J]. Plos one, 2022, 17(10): e0269093.
[4] Podduturi S, Vemula D, Singothu S, et al. In-silico investigation of E8 surface protein of the monkeypox virus to identify potential therapeutic agents[J]. Journal of Biomolecular Structure and Dynamics, 2024, 42(16): 8242-8255.
[5] Kumar R, Wiebe L I, Knaus E E. Synthesis and antiviral activity of novel 5-(1-azido-2-haloethyl) and 5-(1-azido-, amino-, or methoxyethyl) analogs of 2'-deoxyuridine[J]. Journal of medicinal chemistry, 1993, 36(17): 2470-2474.

Edoxudine (EUDR)是一种脱氧胸苷类似物，已被证实对单纯疱疹病毒1型和2型具有抑制作用^[1]。在脊椎动物系统中，Edoxudine可优先被胸苷激酶磷酸化并掺入病毒DNA中，从而抑制病毒DNA的合成^[2]。Edoxudine能破坏肺炎克雷伯菌的外壁并损伤其脂多糖层的保护作用，使细菌细胞膜对抗菌效应物更易感^[3]。Edoxudine已广泛用作先导化合物，用于开发靶向猴痘病毒E8表面蛋白的药物^[4]。

在体外，使用Edoxudine处理人包皮成纤维细胞（HFFs）72小时，显著抑制了细胞增殖，IC₅₀值为115µM ^[5]。