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Cited by 258Prostate Cancer Treatment and ResearchEstrogen and related hormone effectsHormonal and reproductive studies

The DOI matches its Crossref record; 33 of the 33 references it cites were found in a registry or an index.

Characteristics of interaction of the antiandrogen flutamide with the androgen receptor in various target tissues.

Simard, J., Luthy, I., Guay, J., Bélanger, A., Labrie, F.·1986·Molecular and Cellular Endocrinology
DOI 10.1016/0303-7207(86)90132-2
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Abstract

In rat adenohypophysial cells in primary culture, the specific uptake of [3H] testosterone (T) is completely blocked by increasing concentrations of the pure antiandrogen flutamide-OH, the active metabolite of flutamide at an IC50 value of 50 nM while unlabeled T causes a similar inhibition at an IC50 value of 0.5 nM. After 210 min of incubation of 3 nM [3H]T with the anterior pituitary cells, 80% of radioactivity is still present as unchanged T. Direct binding studies show that flutamide-OH and flutamide interact with the rat anterior pituitary androgen receptor at Ki values of 55 and 1275 nM, respectively. In rat ventral prostate (cytosolic and nuclear fractions) and cytosol from human prostatic carcinoma, rat uterus and mouse Shionogi mammary carcinoma, the Ki values ranged from 0.1 to 0.47, 0.6 to 2.7, 62 to 205 and 1450 to 7550 nM for dihydrotestosterone, T, flutamide-OH and flutamide, respectively . Since the ability of flutamide-OH to inhibit the uptake of [3H]T in intact adenohypophysial cells and to compete for binding to the adenohypophysial androgen receptor shows almost identical values at approximately 1% of the potency of T itself, it is most likely that the antiandrogen activity of flutamide-OH can be completely explained by the ability of the pure antiandrogen to displace androgen from their specific receptor in target tissues. In addition, the finding of similar binding characteristics in a series of other tissues suggests that a similar potency of the antiandrogen can be expected in the other androgen-target tissues.

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Crossref · 10.1016/0303-7207(86)90132-2

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Research works printed but not linked: 6

  1. Asselin, 1980, Cancer Res., 40, 1612
  2. Fang, 1969, Mol. Pharmacol., 5, 428
  3. Labrie, 1986, Prostate
  4. Labrie, 1982, J. Clin. Invest. Med., 5, 267
  5. Labrie, 1985, J. Steroid Biochem.
  6. Neumann, 1970, Recent Progr. Horm. Res., 26, 337

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Metadata

Authors
Simard, J., Luthy, I., Guay, J., Bélanger, A., & Labrie, F.
Affiliations
Université Laval (CA)
ORCID
Simard, J.
Venue
Molecular and Cellular Endocrinology
Publisher
Elsevier BV
Published
1986-03
Volume
44
Issue
3
Pages
261-270
ISSN
0303-7207 (ISSN-L)
DOI
10.1016/0303-7207(86)90132-2
OpenAlex
W2036335596
Cited by
256
References
33
Citations by year
2026: 3 · 2025: 6 · 2024: 2 · 2023: 5 · 2022: 5 · 2021: 4 · 2020: 3 · 2019: 1 · 2018: 6 · 2017: 1 · 2016: 5 · 2015: 6 · 2014: 9 · 2013: 7 · 2012: 5
FWCI
26.48
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
  • Fonds de Recherche du Québec - Santé
  • Medical Research Council
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Prostate Cancer Treatment and Research
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Hormonal and reproductive studies
Keywords
flutamide, androgen receptor antagonists, androgen receptor, receptor binding affinity, testosterone uptake, anterior pituitary, ventral prostate, uterus, breast cancer, dihydrotestosterone
MeSH terms
Anilides, Animals, Cells, Cultured, Female, Flutamide, Humans, Kinetics, Male, Mammary Neoplasms, Experimental, Mice, Inbred Strains, Organ Specificity, Pituitary Gland, Anterior, Prostate, Prostatic Neoplasms, Rats, Inbred Strains, Receptors, Androgen, Testosterone, Uterus, Mice, Rats

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