thymidine kinase

3,4,5-Triiodobenzoic acid 是硫嘌呤甲基转移酶 (TPMT) 的抑制剂。

DI-87(TRE-515)是一种新型和可口服的dCK（deoxycytidine kinase）抑制剂，具有良好的体外活性和低蛋白结合率，DI-87与dCK结合后，阻止dCK对脱氧胞苷的磷酸化反应，从而减少dNTP的生成和细胞周期停滞（特别是在S期）。与胸苷联合使用时，DI-87能显著抑制肿瘤生长。

Acyclovir (Aciclovir) 是鸟嘌呤类似物和具有口服活性的抗病毒剂。它对HSV-1(IC50为 0.85 μM)，HSV-2(IC50为 0.86 μM) 和水痘带状疱疹病毒有活性。

Penciclovir (BRL 39123) 是一种疱疹病毒核苷类似物 DNA 聚合酶抑制剂。它作用于HSV1 和 2，IC50分别为 0.04-1.8 μg mL 和 0.06-4.4 μg mL。

DHQ (2,3-dihydroxy-quinoxalin) 是单纯疱疹病毒胸苷激酶的 ATPase 活性诱导剂。

2'-Fluorothymidine(2'-Deoxy-2'-fluoro-5-Methyluridine) 属于胸腺嘧啶 (TdR) 和甲基尿苷的同工酶，是具有高度选择性的 2 型胸苷激酶 (TK2) 的底物。

(S)-DI-87((S)-TRE-515)是DI-87的异构体。DI-87是一种新型和可口服的dCK（deoxycytidine kinase）抑制剂，具有良好的体外活性和低蛋白结合率，DI-87与dCK结合后，阻止dCK对脱氧胞苷的磷酸化反应，从而减少dNTP的生成和细胞周期停滞（特别是在S期）。与胸苷联合使用时，DI-87能显著抑制肿瘤生长。

Carbetimer is a partially imidized copolymer of ethylene & maleic anhydride with average MW approx 1,200 daltons; capable of specific stimulation of immune response. Carbetimer is a low molecular weight polymer derived from ethylene and maleic anhydride with potent antineoplastic activity. Preclinical studies have shown antitumor effects against many tumor cell lines including B 16 melanoma. Its antitumor actions are felt to include both reduction of uridine and cytidine nucleoside triphosphate as well as the diminution of pyrimidine salvage by inhibiting uridine, cytidine, and thymidine kinase. Besides direct antiproliferative effects, Carbetimer could act through immunomodulation, as suggested by the induction of cytotoxic T-cells in mice and the discordant in vitro and in vivo activities against the Lewis lung carcinoma model.

Fazarabine, also known as Kymarabine, is an orally-active pyrimidine analogue of an aza-substituted cytidine in which the ribose moiety is replaced by an arabinose sugar. Similar in action to cytarabine, fazarabine is phosphorylated by deoxycytidine kinase to a triphosphate form which competes with thymidine for incorporation into DNA; its incorporation into DNA inhibits DNA synthesis, resulting in tumor cell death and tumor necrosis. The presence of deoxycytidine kinase in a tumor is a determinant of tumor sensitivity to this drug.

Bucyclovir triphosphate is an antiherpes and cyclic guanosine analog activated by the viral thymidine kinase to inhibit viral DNA synthesis in infected cells.

Thymidine 5′-diphosphate (dTDP) 是合成嘧啶的关键产物，通过胸苷酸激酶 (TMPK) 对 5'-单磷酸胸苷 (dTMP) 进行磷酸化反应生成，此过程需 ATP 与 Mg2+。进一步，dTDP 可被 TMPK 催化转化为胸苷 5'-三磷酸 (dTTP)。通过测量 dTDP 水平，可以评估 TMPK 活性。

BVDU 5′-Triphosphate 是带有 5′-Triphosphate 标记、针对 DNA 聚合酶的抗病毒药物。它对水痘-带状疱疹病毒（VZV）和单纯疱疹病毒 1 型（HSV-1）具有高度选择性，这种选择性归因于病毒编码的胸苷激酶对其进行特异性磷酸化的能力。

TMP-CP（Thymidine-5’-O-(α,β-methylene)diphosphate）是TDP的一种水解稳定衍生物，同时也是一种thymidine kinase抑制剂（Ki = 23 µM）。它已被用作α,β-methylene-2’-deoxythymidine 5’-triphosphate合成的前体，该合成物是DNA polymerase的一种不可切割底物。