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Targeted Covalent Inhibition of Telomerase.
ACS Chemical Biology ( IF 3.5 ) Pub Date : 2020-02-24 , DOI: 10.1021/acschembio.9b00945 Rick C Betori 1 , Yue Liu 2 , Rama K Mishra 3 , Scott B Cohen 4 , Stephen J Kron 2 , Karl A Scheidt 1, 3, 5
ACS Chemical Biology ( IF 3.5 ) Pub Date : 2020-02-24 , DOI: 10.1021/acschembio.9b00945 Rick C Betori 1 , Yue Liu 2 , Rama K Mishra 3 , Scott B Cohen 4 , Stephen J Kron 2 , Karl A Scheidt 1, 3, 5
Affiliation
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Telomerase is a ribonuceloprotein complex responsible for maintaining telomeres and protecting chromosomal integrity. The human telomerase reverse transcriptase (hTERT) is expressed in ∼90% of cancer cells where it confers the capacity for limitless proliferation. Along with its established role in telomere lengthening, telomerase also serves noncanonical extra-telomeric roles in oncogenic signaling, resistance to apoptosis, and enhanced DNA damage response. We report a new class of natural-product-inspired covalent inhibitors of telomerase that target the catalytic active site.
中文翻译：
端粒酶的靶向共价抑制。
端粒酶是一种核糖体蛋白复合物，负责维持端粒并保护染色体完整性。人类端粒酶逆转录酶（hTERT）在约90％的癌细胞中表达，赋予无限增殖能力。端粒酶不仅在端粒延长中起着确定的作用，而且还在致癌信号传导，抗凋亡和增强的DNA损伤反应中发挥非经典的端粒作用。我们报告了靶向催化活性位点的一类新的天然产物启发的端粒酶共价抑制剂。
更新日期：2020-02-24
中文翻译：
端粒酶的靶向共价抑制。
端粒酶是一种核糖体蛋白复合物，负责维持端粒并保护染色体完整性。人类端粒酶逆转录酶（hTERT）在约90％的癌细胞中表达，赋予无限增殖能力。端粒酶不仅在端粒延长中起着确定的作用，而且还在致癌信号传导，抗凋亡和增强的DNA损伤反应中发挥非经典的端粒作用。我们报告了靶向催化活性位点的一类新的天然产物启发的端粒酶共价抑制剂。
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