1. Signaling Pathways
  2. Apoptosis
  3. Thymidylate Synthase

Thymidylate Synthase (胸苷酸合成酶)

Thymidylate synthase (TS) is an E2F1-regulated enzyme that is essential for DNA synthesis and repair. Thymidylate synthase is an essential S phase enzyme required for DNA synthesis. Thymidylate synthase plays a central role in the biosynthesis of thymidylate, an essential precursor for DNA synthesis.

Thymidylate synthase catalyzes the reductive methylation of 2′-deoxyuridine 5-monophosphate (dUMP) by transfer of a methylene group from a cofactor, CH2H4 folate, to generate deoxythymidine-5′-monophoshate (dTMP). dTMP is further phosphorylated to the triphosphate state (dTTP), which is a direct precursor for DNA synthesis. Since the TS catalyzed reaction is the sole intracellular de novo source of dTMP, the inhibition of TS results in the cessation of cellular proliferation and growth.

Thymidylate synthase protein and mRNA levels are elevated in many human cancers, and high TS levels have been correlated with poor prognosis in patients with colorectal, breast, cervical, bladder, kidney, and non-small cell lung cancers.

Thymidylate Synthase 相关产品 (7):

目录号 产品名 作用方式 纯度
  • HY-10821
    Raltitrexed Inhibitor ≥98.0%
  • HY-16478
    Trifluridine/tipiracil hydrochloride mixture Inhibitor ≥98.0%
    Trifluridine-tipiracil hydrochloride mixture (TAS-102) 是一种新型的口服组合药物。由基于胸苷的抗肿瘤核苷类似物,三氟胸苷和有效的胸苷磷酸化酶 (thymidine phosphorylase) 抑制剂派替西西以1比0.5比例组成。
  • HY-A0061
    Trifluridine Inhibitor 99.85%
    Trifluridine (Trifluorothymidine; 5-Trifluorothymidine; TFT) 是不可逆的胸苷酸合酶抑制剂,从而抑制 DNA合成。Trifluridine 是用于单纯疱疹病毒 (HSV) 感染的抗病毒药物。
  • HY-A0063A
    Tipiracil Inhibitor
    Tipiracil 是一种胸苷磷酸化酶 (TPase) 抑制剂。
  • HY-108474
    Nolatrexed dihydrochloride Inhibitor 98.21%
    Nolatrexed dihydrochloride (AG 337) 是一种非竞争性的胸苷酸合酶 (thymidylate synthase) 抑制剂,与该酶的叶酸辅因子结合位点相互作用,对人 thymidylate synthase 的 Ki 值为 11 nM。Nolatrexed dihydrochloride (AG 337) 能够在癌细胞 S 期诱导细胞周期停滞。具有抗癌活性。
  • HY-13728
    Plevitrexed Inhibitor
    Plevitrexed (ZD 9331; BGC9331) 是口服有效的胸苷酸合酶 (TS) 抑制剂,Ki 值为 0.44 nM。Plevitrexed 通过 α-叶酸受体以及还原的叶酸载体吸收。Plevitrexed 有用于胃癌的潜力。
  • HY-13728B
    (Rac)-Plevitrexed Inhibitor
    (Rac)-Plevitrexed ((Rac)-ZD 9331; (Rac)-BGC9331) 是 Plevitrexed 的外消旋体。Plevitrexed 是口服有效的胸苷酸合酶 (TS) 抑制剂。
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