Recent advances of tyrosyl-DNA phosdiesterase Ⅰ (TdpⅠ) inhibitors
10.3969/j.issn.1006-0111.2015.04.003
- VernacularTitle:酪氨酸-DNA磷酸二酯酶抑制剂的研究进展
- Author:
Yahui HUANG
1
;
Guoqiang DONG
;
Wannian ZHANG
;
Chunquan SHENG
Author Information
1. 第二军医大学药学院
- Keywords:
tyrosyl-DNA phosphodiesterase Ⅰ (TdpⅠ);
topoisomerase Ⅰ (TopⅠ);
anti-tumor inhibitors;
structure and activity relationship
- From:
Journal of Pharmaceutical Practice
2015;(4):298-302
- CountryChina
- Language:Chinese
-
Abstract:
Tyrosyl-DNA phosphodiesterase Ⅰ (TdpⅠ ) is a recently discovered proteinthat catalyzes the hydrolysis of 3′-phosphotyrosyl bonds .Such linkages form in vivo during the interaction of DNA and topoisomerase Ⅰ (TopⅠ) .TdpⅠ has been regarded as a potential therapeutic co-target of TopⅠ because it has the functions of repairing Top Ⅰ compound and coun-teracting the effects of Top Ⅰ inhibitors .TdpⅠ inhibitors can not only synergizing with Top Ⅰ-targeting drugs (camptoth-ecins) ,but also strength the function of bleomycin ,topoisomerase Ⅱ (TopⅡ ) inhibitors (etoposide ,doxorubicin) and DNA alkylating agents .We summarized the researching advance of TdpⅠ inhibitors and focused on the introduction of the mecha-nism ,bioactivity and structure-activity relationship .
