Inhibition of poly(ADP-ribose) polymerase by nucleic acid metabolite 7-methylguanine
| العنوان: | Inhibition of poly(ADP-ribose) polymerase by nucleic acid metabolite 7-methylguanine |
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| المؤلفون: | Nilov, D. K., Tararov, V. I., Kulikov, A. V., Zakharenko, A. L., Gushchina, I. V., Mikhailov, S. N., Lavrik, O. I., Vytas Svedas |
| المصدر: | ResearcherID Scopus-Elsevier |
| بيانات النشر: | Общество с ограниченной ответственностью Парк-медиа, 2016. |
| سنة النشر: | 2016 |
| مصطلحات موضوعية: | PARP INHIBITORS,MOLECULAR MODELING,DOCKING |
| الوصف: | The ability of 7-methylguanine, a nucleic acid metabolite, to inhibit poly (ADP-ribose) polymerase-1 (PARP-1) and poly(ADP-ribose)polymerase-2 (PARP-2) has been identified in silico and studied experimentally.The amino group at position 2 and the methyl group at position 7 were shown to be important substituents for the efficient binding of purine derivatives to PARPs. The activity of both tested enzymes, PARP-1 and PARP-2, was suppressed by 7-methylguanine with IC50 values of 150 and 50 μM, respectively. At the PARP inhibitory concentration, 7-methylguanine itself was not cytotoxic, but it was able to accelerate apoptotic death of BRCA1-deficient breast cancer cells induced by cisplatin and doxorubicin, the widely used DNA-damaging chemotherapeutic agents. 7-Methylguanine possesses attractive predictable pharmacokinetics and an adverse-effect profile and may be considered as a new additive to chemotherapeutic treatment. |
| وصف الملف: | text/html |
| اللغة: | Russian |
| تدمد: | 2075-8251 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=dedup_wf_001::409588b8bbd064a103386b8657b4f6e9Test http://cyberleninka.ru/article/n/inhibition-of-poly-adp-ribose-polymerase-by-nucleic-acid-metabolite-7-methylguanineTest |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.dedup.wf.001..409588b8bbd064a103386b8657b4f6e9 |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 20758251 |
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