ArticleJournal of medicinal chemistry2015
Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity.
Article in Journal of medicinal chemistry, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 118 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
118 citing papers in PubMed, 192 citations in OpenAlex.
- Exendin-4 averts all-trans-retinal-driven damage to photoreceptors and the retina via the GLP-1R/PKA/CREB1 signaling axis.Cellular & molecular biology letters · 2026Article
- WAT-to-BAT communication facilitates the sustained activation of BAT thermogenesis during cold exposure.Cell discovery · 2026Article
- Dormancy exit correlates with CREB1 reactivation that is a potential target to overcome endocrine therapy resistance in ERiScience · 2026Article
- Molecular mechanisms by which tumor cell CD73-mediated adenosine signaling drives M2 polarization of macrophages in non-small cell lung cancer.Frontiers in cell and developmental biology · 2026Article
- Design, synthesis and evaluation of clickable photoaffinity probes for nuclear lamins.Bioorganic & medicinal chemistry letters · 2025Article
- Discovery of peptidomimetic inhibitors of CREB/CBP by targeting hydrophobic grooves on the surface of the CBP KIX domain.Acta pharmaceutica Sinica. B · 2025Article
- Development of a CRE/CREB-driven HBx responsive HBV cell culture reporter system for antiviral drug evaluation.JHEP reports : innovation in hepatology · 2025Article
- Phosphodiesterase Inhibition Increases Striatal GDNF and Protects Against Preclinical Parkinsonism.Journal of neurochemistry · 2025Article
- A time-gated PKA-CREB signaling circuit licenses IL-12 responsiveness and Th1 fate in CD4Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Article
- EF1α, rather than CMV promoter, is suitable for luciferase tag expression in target cells forMolecular therapy. Methods & clinical development · 2025Article
- Tandem association of CLOCK:BMAL1 complexes on DNA enables recruitment of CBP/p300 through multivalent interactions.bioRxiv : the preprint server for biology · 2025Article
- Dynamic Ca2+-Dependent Transcription Links Metabolic Stress to Impaired β-Cell Identity.Diabetes · 2025Article
- Microglial BDNF modulates arketamine's antidepressant-like effects through cortico-accumbal pathways.Science advances · 2025Article
- Cholesterol metabolism regulated by CAMKK2-CREB signaling promotes castration-resistant prostate cancer.Cell reports · 2025Article
- NSC632839 suppresses esophageal squamous cell carcinoma cell proliferation in vitro by triggering spindle assembly checkpoint-mediated mitotic arrest and CREB-Noxa-dependent apoptosis.Cancer cell international · 2025Article
- The universal role of adaptive transcription in health and disease.The FEBS journal · 2025Review
- Multi-omics profiling reveals key factors involved in Ewing sarcoma metastasis.Molecular oncology · 2025Article
- cAMP response element-binding protein: A credible cancer drug target.The Journal of pharmacology and experimental therapeutics · 2025Review
- Stress and Obesity Signaling Converge on CREB Phosphorylation to Promote Pancreatic Cancer.Molecular cancer research : MCR · 2025Article
58 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 1 institution in 1 country.
Funding
Abstract
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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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.