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Your search keyword '"Zhao, Yining"' showing total 2 results
Start Over Author "Zhao, Yining" Journal chemico-biological interactions
2 results on '"Zhao, Yining"'

1. In vitro CAPE inhibitory activity towards human AKR1C3 and the molecular basis.

Author

Li, Cuiyun, Zhao, Yining, Zheng, Xuehua, Zhang, Hong, Zhang, Liping, Chen, Yunyun, Li, Qing, and Hu, Xiaopeng

Subjects
*PROSTATE cancer treatment, *ALDO-keto reductases, *CAFFEIC acid, *PHENOLIC acids, *X-ray crystallography, *IN vitro studies
Abstract

AKR1C3 is a critical enzyme for producing testosterone and 5α-DHT in the human body. Inhibiting AKR1C3 is a potential target for treating castration-resistant prostate cancer (CRPC). To find AKR1C3 inhibitors with a new molecular skeleton and binding mode, we analyzed the in vitro inhibitory activity of caffeic acid phenethyl ester (CAPE) and eight other phenolic acid analogues towards AKR1C3 and six other human AKR1 enzymes. We analyzed CAPE and octyl gallate interactions with AKR1C3 using X-ray crystallography, which provided a molecular basis for understanding the phenolic acid inhibitory activity and selectivity towards human AKR1s. [ABSTRACT FROM AUTHOR]

Published
2016
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2. In vitro inhibition of AKR1Cs by sulphonylureas and the structural basis.

Author

Zhao, Yining, Zheng, Xuehua, Zhang, Hong, Zhai, Jing, Zhang, Liping, Li, Cuiyun, Zeng, Kaixin, Chen, Yunyun, Li, Qing, and Hu, Xiaopeng

Subjects
*CANCER chemotherapy, *X-rays, *DRUG therapy, *CANCER treatment, *ELECTROMAGNETIC waves
Abstract

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. [ABSTRACT FROM AUTHOR]

Published
2015
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