"Drug screening to target nuclear orphan receptor NR4A2 for cancer ther" by Takefumi Komiya MD, Satomi Yamamoto et al.
 

Drug screening to target nuclear orphan receptor NR4A2 for cancer therapeutics.

Abstract

Background: Our previous study suggested NR4A2, a subfamily member of orphan nuclear receptors, is essential for survival of human cancer cells such as mucoepidermoid carcinoma (MEC).

Methods: We conducted high throughput drug screening for NR4A2 inhibitors as a novel therapeutic modality. Positive screening was performed using a luciferase reporter vector containing NR4A2 binding sequence, and a CRE-reporter control vector was used to eliminate false positives. In vitro assays for positive hits were conducted.

Results: A total of 23 Food and Drug Administration (FDA) and 43 Life Science Library compounds were identified, including several epidermal growth factor inhibitors and Src inhibitors. Subsequent

Conclusions: Further research should focus on homologue selectivity,

Document Type

Article

Publication Date

10-1-2017

Publication Title

Transl Lung Cancer Res

First Page

600

Last Page

610

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