The DOI matches its Crossref record; 36 of the 36 references it cites were found in a registry or an index.
CDB-4124 and its putative monodemethylated metabolite, CDB-4453, are potent antiprogestins with reduced antiglucocorticoid activity: in vitro comparison to mifepristone and CDB-2914
Abstract
To obtain selective antiprogestins, we have examined the in vitro antiprogestational/antiglucocorticoid properties of two novel compounds, CDB-4124 and the putative monodemethylated metabolite, CDB-4453, in transcription and receptor binding assays and compared them to CDB-2914 and mifepristone. All four antiprogestins bound with high affinity to rabbit uterine progestin receptors (PR) and recombinant human PR-A and PR-B (rhPR-A, rhPR-B) and were potent inhibitors of R5020-induced transactivation of the PRE2-tk-luciferase (PRE2-tk-LUC) reporter plasmid and endogenous alkaline phosphatase production in T47D-CO human breast cancer cells. None of these compounds exhibited agonist activity in these cells. Induction of luciferase activity was potentiated about five-fold by 8-Br-cAMP under basal conditions and to the same extent in the presence of the PR antagonists. Mifepristone bound to rabbit thymic glucocorticoid receptors (GR) with approximately twice the avidity of the CDB antiprogestins. Inhibition of GR-mediated transcription of PRE2-tk-LUC was assessed in HepG2 human hepatoblastoma cells. Mifepristone exhibited greater antiglucocorticoid activity than CDB-2914, 4124, and 4453, about 12-, 22-, and 185-fold, respectively. Thus, while there was a good correlation between binding to PR and functional activity of these antiprogestins, GR binding was not predictive of their glucocorticoid antagonist activity. In agreement with our in vivo results, CDB-4124 and CDB-4453, as well…
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“CDB-4124 is a PR antagonist with a low binding affinity for glucocorticoid receptors [13]”
From Sex-specific effects of neonatal progestin receptor antagonism on juvenile social play behavior in rats (2021) · cites this paper as [13]
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Metadata
- Authors
- Attardi, B. J., Burgenson, J., Hild, S. A., Reel, J. R., & Blye, R. P.
- Affiliations
- Bioqual (US)
- Eunice Kennedy Shriver National Institute of Child Health and Human Development (US)
- Corresponding author
- Attardi, Barbara J.
- Venue
- Molecular and Cellular Endocrinology
- Publisher
- Elsevier BV
- Published
- 2002-02
- Volume
- 188
- Issue
- 1-2
- Pages
- 111-123
- ISSN
- 0303-7207 (ISSN-L)
- OpenAlex
- W2045180596
- Cited by
- 118
- References
- 36
- Citations by year
- 2026: 3 · 2024: 1 · 2023: 1 · 2022: 3 · 2021: 9 · 2020: 4 · 2019: 5 · 2018: 2 · 2017: 3 · 2016: 6 · 2015: 4 · 2014: 12 · 2013: 6 · 2012: 9
- FWCI
- 1.41
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Molecular and Cellular Endocrinology (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Eunice Kennedy Shriver National Institute of Child Health and Human Development (N01-HD-6-3259)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Reproductive Health and Contraception
- Physical Sciences › Chemistry › Organic Chemistry › Heterocyclic Compound Synthesis and Bioactivity
- Keywords
- mifepristone, antiprogestins, antiglucocorticoid activity, progestin receptor, glucocorticoid receptor, receptor binding, transcriptional activation, drug metabolites, breast cancer cells, hepatoblastoma cells
- MeSH terms
- Alkaline Phosphatase, Animals, Binding, Competitive, Enzyme Induction, Hormone Antagonists, Luciferases, Norpregnadienes, Plasmids, Progestins, Rabbits, Receptors, Androgen, Receptors, Glucocorticoid, Receptors, Progesterone, Recombinant Proteins, Transfection, Tumor Cells, Cultured, 8-Bromo Cyclic Adenosine Monophosphate, Transcriptional Activation, Mifepristone, Rats
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