1. Signaling Pathways
  2. Apoptosis
  3. Thymidylate Synthase

Thymidylate Synthase (胸苷酸合成酶)

Thymidylate synthase (TSase) is a key enzyme in cell proliferation as it catalyzes a reaction essential for DNA replication, a reductive methylation of 2′-deoxyuridine-5′-monophosphate (dUMP) to form 2′-deoxythymidine-5′-monophosphate (dTMP) using the co-substrate N5,N10-methylene-5,6,7,8-tetrahydrofolate (CH2H4F).

The activity and expression of TSase are tightly controlled throughout the cell cycle, particularly at the translational level. The TSase protein itself binds to the TSase mRNA both at the translational start site (TSS) and in the coding region, inhibiting translational processing of the message. TSase can also bind to the mRNA of at least nine other important gene products, including those of p53 and c-myc. Therefore, manipulating the level of the TSase protein could induce a cascade of consequential effects on cell growth. Because of its importance in DNA precursor synthesis and repair, TSase has proved to be an important target for many chemotherapeutic and antibiotic drugs. Structural analogs of dUMP (e.g., fluoropyrimidines) and CH2H4F (e.g., antifolates) are well-established drugs targeting thymidylate synthase.

Thymidylate Synthase 相关产品 (12):

目录号 产品名 作用方式 纯度
  • HY-16478
    Trifluridine/tipiracil hydrochloride mixture Inhibitor ≥98.0%
    Trifluridine/tipiracil hydrochloride mixture (TAS-102) 是一种有效且具有口服活性的核苷类抗肿瘤剂。Trifluridine/tipiracil hydrochloride mixture (TAS-102) 的组成是 1:0.5 的混合物 (以摩尔计) α,α,α-三氟胸苷 (FTD) 和胸苷磷酸化酶抑制剂 (TPI)。Trifluridine/tipiracil hydrochloride mixture (TAS-102) 主要通过抑制胸苷酸合酶 (TS) 和掺入 DNA 来显示抗肿瘤活性。
  • HY-10821
    Raltitrexed

    雷替曲塞

    Inhibitor ≥98.0%
    Raltitrexed是一种用于化疗的抗代谢药物,通过抑制胸苷酸合成酶起作用。
  • HY-A0061
    Trifluridine

    曲氟尿苷

    Inhibitor 99.72%
    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

    替吡嘧啶

    Inhibitor
    Tipiracil 是一种胸苷磷酸化酶 (TPase) 抑制剂。
  • HY-108474
    Nolatrexed dihydrochloride

    盐酸诺拉曲塞; 诺拉曲塞盐酸盐

    Inhibitor 98.54%
    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-143207
    10-Formyl-5,8-dideazafolic acid Inhibitor
    10-Formyl-5,8-dideazafolic acid 是一种胸苷酸合成酶 (thymidylate synthase) 抑制剂。
  • HY-109115
    Fosifloxuridine nafalbenamide Inhibitor 98.18%
    Fosifloxuridine nafalbenamide (NUC-3373) 属于嘧啶核苷酸类似物,是一种胸腺嘧啶合酶 (Thymidylate synthase) 抑制剂。Fosifloxuridine nafalbenamide 具有抗癌活性。Fosifloxuridine nafalbenamide 具有诱发宿主免疫反应和增强免疫治疗的潜力。
  • HY-10822
    Idetrexed Inhibitor
    Idetrexed 是一种胸腺嘧啶合成酶抑制剂,特异性转运到 α 叶酸受体 (α - fr) 过表达肿瘤。Idetrexed 在 1.2 nmol/L 时抑制胸腺苷酸合成酶 a。
  • HY-13728
    Plevitrexed

    普来曲塞

    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

    (Rac)-普来曲塞

    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。
  • HY-10822A
    ONX 0801 trisodium Inhibitor
    ONX 0801 (BGC 945) trisodium 是胸腺激酶合成酶 (TS) 的抑制剂,靶向α 叶酸受体过表达的肿瘤。
  • HY-108474S
    Nolatrexed-d4 dihydrochloride

    盐酸诺拉曲塞 d4 (双盐酸盐)

    Inhibitor
    Nolatrexed-d4 dihydrochloride 是 Nolatrexed dihydrochloride 的氘代物。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。
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