In vitro inhibition of AKR1Cs by sulphonylureas and the structural basis

被引：34
作者：
Zhao, Yining [1 ,2 ]
Zheng, Xuehua [1 ,2 ]
Zhang, Hong [1 ,2 ]
Zhai, Jing [1 ,2 ]
Zhang, Liping [1 ,2 ]
Li, Cuiyun [1 ,2 ]
Zeng, Kaixin [1 ,2 ]
Chen, Yunyun [1 ,2 ]
Li, Qing [1 ,2 ]
Hu, Xiaopeng [3 ]
机构：
[1] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China
[2] Sun Yat Sen Univ, Ctr Cellular & Struct Biol, Guangzhou 510006, Guangdong, Peoples R China
[3] Biopolcore Inc, Baltimore, MD 21221 USA
来源：
CHEMICO-BIOLOGICAL INTERACTIONS | 2015年 / 240卷
关键词：
Sulphonylureas; AKR1Cs; Inhibition; Selectivity; Crystal structures; PROSTAGLANDIN-F-SYNTHASE; AMERICAN-DIABETES-ASSOCIATION; CRYSTAL-STRUCTURE; EUROPEAN ASSOCIATION; STEROID-HORMONE; CANCER; METFORMIN; METABOLISM; EXPRESSION; RISK;
D O I：
10.1016/j.cbi.2015.09.006
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Recent epidemiological studies show conflicting data for the first-line anti-diabetic sulphonylureas drugs in treating cancer progression in type II diabetes patients. How sulphonylureas promote or diminish tumor growth is not fully understood. Here, we report that seven sulphonylureas exhibit different in vitro inhibition towards AKR1Cs (AKR1C1, AKR1C2, AKR1C3), which are critical steroid hormone metabolism enzymes that are related to prostate cancer, breast cancer and endometrial diseases. Interactions of the sulphonylureas and AKR1Cs were analyzed by X-ray crystallography. (C) 2015 Elsevier Ireland Ltd. All rights reserved.
引用
收藏
页码：310 / 315
页数：6
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