1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. Telomerase

Telomerase (端粒酶)

端粒酶 (Telomerase) 是一种 DNA 聚合酶,它通过连续合成多个端粒重复序列来延伸染色体的 3' 端。它是一种独特的核糖核蛋白 (RNP),含有专门的端粒酶逆转录酶 (TERT) 和端粒酶 RNA (TER),具有自己的模板和 TERT 活性所需的其他元素(催化核心),以及对生物合成和组装很重要的物种特异性 TER 结合蛋白(核心 RNP);其他蛋白质暂时或组成性地结合端粒酶,使端粒酶和其他蛋白质与端粒末端结合,从而调节 DNA 合成。

端粒酶活性负责维持大多数人类恶性肿瘤中的染色体末端结构(端粒)和癌细胞永生,使端粒酶成为一个有吸引力的治疗靶点。事实上,端粒酶抑制剂有望在大多数癌症中提供治疗益处,同时副作用很小。正常组织中表达端粒酶的成体干细胞分裂缓慢,端粒较长,因此,与分裂迅速、端粒通常较短的癌细胞相比,它们受端粒酶抑制的影响较小。

Telomerase is a DNA polymerase that extends the 3' ends of chromosomes by processively synthesizing multiple telomeric repeats. It is a unique ribonucleoprotein (RNP) containing a specialized telomerase reverse transcriptase (TERT) and telomerase RNA (TER) with its own template and other elements required with TERT for activity (catalytic core), as well as species-specific TER-binding proteins important for biogenesis and assembly (core RNP); other proteins bind telomerase transiently or constitutively to allow association of telomerase and other proteins with telomere ends for regulation of DNA synthesis.

Telomerase activity is responsible for the maintenance of chromosome end structures (telomeres) and cancer cell immortality in most human malignancies, making telomerase an attractive therapeutic target. Indeed, a telomerase inhibitor is expected to provide a therapeutic benefit in most cancers while having little side-effects. The adult stem cells that express telomerase in normal tissues divide slowly and have long telomeres, therefore they should be less impacted by telomerase inhibition than the cancer cells which divide rapidly and usually possess short telomeres.

Telomerase 相关产品 (46):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-129334
    Macrocalin B Inhibitor
    Macrocalin B 是一种二萜类化合物,可从 Isodon xerophilus 中分离得到。Macrocalin B 抑制癌细胞 K562、HL-60、A549、MKN、CA 和 HCT 的增殖,IC50 为 2.81-171 μM。Macrocalin B 抑制 K562 中的端粒酶 (telomerase) 活性,IC50 为纳摩尔水平。
    Macrocalin B
  • HY-175103
    Guanine-2'-deoxy-β-L-ribofuranosyl-5'-O-triphosphate sodium Inhibitor
    Guanine-2'-deoxy-β-L-ribofuranosyl-5'-O-triphosphate (sodium) 是 dGTP 的异构体,也是端粒酶 (telomerase) 的抑制剂,对人类酶的 Ki 为 15 μM。
    Guanine-2'-deoxy-β-L-ribofuranosyl-5'-O-triphosphate sodium
  • HY-171573
    3′-Azido-2′,3′-dideoxy-GTP Inhibitor
    3′-Azido-2′,3′-dideoxy-GTP (AZddGTP) 是一种选择性端粒酶抑制剂,Ki 值为 1.5 μM。3′-Azido-2′,3′-dideoxy-GTP 能被端粒酶整合到 DNA 3′ 末端。3′-Azido-2′,3′-dideoxy-GTP 在体外可抑制 HeLa 细胞端粒酶活性。
    3′-Azido-2′,3′-dideoxy-GTP
  • HY-48625
    L2H2-6OTD intermediate-2 Inhibitor 99.72%
    L2H2-6OTD intermediate-2 是一种端粒酶抑制剂的合成中间体,可用于合成 ADC。
    L2H2-6OTD intermediate-2
  • HY-17423R
    Abacavir (Standard)

    阿巴卡韦(Standard)

    Inhibitor
    Abacavir (Standard)是 Abacavir 的分析标准品。本产品用于研究及分析应用。Abacavir 是一种具有口服活性、竞争性核苷酸逆转录酶 (nucleoside reverse transcriptase) 抑制剂。 Abacavir 可抑制 HIV 的复制。Abacavir 在前列腺癌细胞系中显示出抗癌活性。Abacavir 可突破血脑屏障,抑制端粒酶 (telomerase) 活性。
    Abacavir (Standard)
  • HY-N14945
    Diazaphilonic acid

    二扎菲酮酸

    Inhibitor
    Diazaphilonic acid 可由 Talaramuces flavus PF1195 菌株产生。Diazaphilonic acid 没有抗菌活性,但能抑制 DNA 扩增和端粒酶的能力。
    Diazaphilonic acid