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Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity
Open accessAbstract
Recent studies have shown that nuclear transcription factor cyclic adenosine monophosphate response element binding protein (CREB) is overexpressed in many different types of cancers. Therefore, CREB has been pursued as a novel cancer therapeutic target. Naphthol AS-E and its closely related derivatives have been shown to inhibit CREB-mediated gene transcription and cancer cell growth. Previously, we identified naphthamide 3a as a different chemotype to inhibit CREB's transcription activity. In a continuing effort to discover more potent CREB inhibitors, a series of structural congeners of 3a was designed and synthesized. Biological evaluations of these compounds uncovered compound 3i (666-15) as a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM). 666-15 also potently inhibited cancer cell growth without harming normal cells. In an in vivo MDA-MB-468 xenograft model, 666-15 completely suppressed the tumor growth without overt toxicity. These results further support the potential of CREB as a valuable cancer drug target.
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How Chemoproteomics Can Enable Drug Discovery and Development
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Cited by
Chong, C.-M., Ke, M., Tan, Y., Huang, Z., Zhang, K., Ai, N., Ge, W., Qin, D., Lu, J.-H., & Su, H. (2018) · Cell Death & Disease · doi:10.1038/s41419-018-0945-7 · Cited by 66
SMOC1 is a glucose-responsive hepatokine and therapeutic target for glycemic control
Montgomery, M. K., Bayliss, J., Devereux, C., Bezawork-Geleta, A., Roberts, D., Huang, C., Schittenhelm, R. B., Ryan, A., Townley, S. L., Selth, L. A., et al. (2020) · Science Translational Medicine · doi:10.1126/scitranslmed.aaz8048 · Cited by 63
Gritti, I., Wan, J., Weeresekara, V., Vaz, J. M., Tarantino, G., Bryde, T. H., Vijay, V., Kammula, A. V., Kattel, P., Zhu, S., et al. (2025) · Cancer Discovery · doi:10.1158/2159-8290.cd-24-0634 · Cited by 20
Metadata
- Authors
- Xie, F., Li, B. X., Kassenbrock, A., Xue, C., Wang, X., Qian, D. Z., Sears, R. C., & Xiao, X.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2015-06-05
- Volume
- 58
- Issue
- 12
- Pages
- 5075-5087
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W919763026
- Cited by
- 179
- References
- 4
- FWCI
- 3.90
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Xie, F., Li, B. X., Kassenbrock, A., Xue, C., Wang, X., Qian, D. Z., Sears, R. C., & Xiao, X. (2015). Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.5b00468
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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