Cited by 118Estrogen and related hormone effectsReproductive Health and ContraceptionHeterocyclic Compound Synthesis and Bioactivity

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CDB-4124 and its putative monodemethylated metabolite, CDB-4453, are potent antiprogestins with reduced antiglucocorticoid activity: in vitro comparison to mifepristone and CDB-2914

Attardi, Barbara J., Burgenson, Janet, Hild, Sheri A., Reel, Jerry R., Blye, Richard P.·2002·Molecular and Cellular Endocrinology

DOI 10.1016/s0303-7207(01)00743-2

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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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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)
DOI: 10.1016/s0303-7207(01)00743-2
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
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
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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CDB-4124 and its putative monodemethylated metabolite, CDB-4453, are potent antiprogestins with reduced antiglucocorticoid activity: in vitro comparison to mifepristone and CDB-2914

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