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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