French
Deutschمهارکننده توپوایزومراز - ویکی‌پدیا، دانشنامهٔ آزاد
مهارکننده‌های توپوایزومراز(به انگلیسی: Topoisomerase inhibitor) ترکیبات شیمیایی هستند که عملکرد توپوایزومرازها را مسدود می‌کنند[۱] (توپوایزومراز I و II)، آنزیم‌هایی هستند که تغییرات در ساختار DNA را با کاتالیز فرایند شکستن و اتصال مجدد ساختار فسفودی‌استر رشته‌های DNA در چرخه سلولی عادی، کنترل می‌کنند.
در سال‌های اخیر، توپوایزومرازها به عنوان هدف در شیمی درمانی سرطان مورد توجه قرا گرفته‌اند. تصور می‌شود که مهارکننده‌های توپوایزومراز مرحله لیگاز شدن چرخه سلولی را مسدود می‌کنند و باعث ایجاد وقفه‌های تک و دو رشته‌ای می‌شوند که به یکپارچگی ژنوم آسیب می‌رسانند. این وقفه‌ها، متعاقباً منجر به آپوپتوز و مرگ سلولی می‌شود.
مهارکننده‌های توپوایزومراز همچنین می‌توانند به عنوان عوامل ضد باکتری عمل کنند.[۲] کوینولون‌ها (از جمله اسید نالیدکسیک و سیپروفلوکساسین) این عملکرد را دارند. [۳]
منابع[ویرایش]
- ↑ "Definition of topoisomerase inhibitor - NCI Dictionary of Cancer Terms".
- ↑ Mitscher, Lester A. (2005). "Bacterial Topoisomerase Inhibitors: Quinolone and Pyridone Antibacterial Agents". Chemical Reviews. 105 (2): 559–92. doi:10.1021/cr030101q. PMID 15700957.
- ↑ Fisher, L. Mark; Pan, Xiao-Su (2008), "Methods to Assay Inhibitors of DNA Gyrase and Topoisomerase IV Activities", New Antibiotic Targets, Methods In Molecular Medicine, vol. 142, pp. 11–23, doi:10.1007/978-1-59745-246-5_2, ISBN 978-1-58829-915-4, PMID 18437302
کتابشناسی[ویرایش]
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{{cite journal}}: نگهداری یادکرد:نام‌های متعدد:فهرست نویسندگان (link) - Nagarajan M.; Morrell A.; Ioanoviciu A.; Antony S.; Kohlhagen G.; Hollingshead M.; Pommier Y.; Cushman M. (2006). "Synthesis and Evaluation of Indenoisoquinoline Topoisomerase I Inhibitors Substituted with Nitrogen Heterocycles". J. Med. Chem. 49 (21): 6283–6289. doi:10.1021/jm060564z. PMC 2526314. PMID 17034134.