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Komiya T, Yamamoto S, Roy A, et al. Drug screening to target nuclear orphan receptor NR4A2 for cancer therapeutics. Transl Lung Cancer Res. 2017;6(5):600-610doi: 10.21037/tlcr.2017.07.02.
Komiya, T., Yamamoto, S., Roy, A., McDonald, P., & Perez, R. P. (2017). Drug screening to target nuclear orphan receptor NR4A2 for cancer therapeutics. Translational lung cancer research, 6(5), 600-610. https://doi.org/10.21037/tlcr.2017.07.02
Komiya, Takefumi, et al. "Drug screening to target nuclear orphan receptor NR4A2 for cancer therapeutics." Translational lung cancer research vol. 6,5 (2017): 600-610. doi: https://doi.org/10.21037/tlcr.2017.07.02
Komiya T, Yamamoto S, Roy A, McDonald P, Perez RP. Drug screening to target nuclear orphan receptor NR4A2 for cancer therapeutics. Transl Lung Cancer Res. 2017 Oct;6(5):600-610. doi: 10.21037/tlcr.2017.07.02. PMID: 29114475; PMCID: PMC5653521.
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Transl Lung Cancer Res. 2017 Oct;6(5):600-610. doi: 10.21037/tlcr.2017.07.02.

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

Translational lung cancer research

Takefumi Komiya, Satomi Yamamoto, Anuradha Roy, Peter McDonald, Raymond P Perez

Affiliations

  1. Division of Medical Oncology, University of Kansas Medical Center, Fairway, KS, USA.
  2. Section of Hematology/Oncology, Tulane University School of Medicine, New Orleans, LA, USA.
  3. High Throughput Screening Facility, University of Kansas School of Pharmacy, Lawrence, KS, USA.

PMID: 29114475 PMCID: PMC5653521 DOI: 10.21037/tlcr.2017.07.02

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,

Keywords: NR4A2; cAMP responsive element binding (CREB)-regulated transcription coactivator 1-Mastermind-like protein 2 (CRTC1-MAML2); drug screening; mucoepidermoid carcinoma (MEC); non-small cell lung cancer (NSCLC)

Conflict of interest statement

Conflicts of Interest: RP Perez is currently employed by Bristol-Myers Squibb; the other authors have no conflicts of interest to declare.

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