PMID: 6165779Mar 1, 1981Paper

Corticoids and cultured human epidermal keratinocytes: specific intracellular binding and clinical efficacy

The Journal of Investigative Dermatology
M PonecE R De Kloet

Abstract

Cytosol of cultured human epidermal keratinocytes contains macromolecules, that bind corticoids with high affinity. Binding constants were in the same range for cultured keratinocytes originating from different individuals and did not change during serial cell cultivation. At 0 degree C and using 3H-triamcinolone acetonide as ligand, we obtained the following values; apparent Bmax = 160- 250 fmoles/mg protein and Kdiss = 3.1-5.0 nM; with 3H-dexamethasone Bmax = 200-350 fmoles/mg protein, Kdiss = 6.0-11.1 nM, and with 3H-hydrocortisone Bmax = 140-220 fmoles/mg protein, Kdiss = 17-25 nM. There was an indication that the binding capacity of the receptor system is higher the younger the age of the skin donor. A number of steroids and corticoids commonly used in dermatological practice were tested with respect to displacement of 3H-triamcinolone acetonide, 3H-dexamethasone, and 3H-hydrocortisone from binding sites in cytosol. Good correlation between clinical efficacy and specific binding was observed for all 3 ligands. Other steroids such as 17-beta estradiol and nandrolone did not show any affinity for the corticoid binding system. Progesterone displace 3H-corticoids from their binding sites, but the IC50 was of one order of magni...Continue Reading

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Citations

Jan 1, 1986·Archives of Dermatological Research·M Ponec, M L Williams
Jan 1, 1985·Clinical and Experimental Dermatology·S M HardingM J Busse
Jan 1, 1984·International Journal of Dermatology·M Ponec
Jul 1, 1984·The British Journal of Dermatology·J F NorrisS Forster
May 27, 1997·Proceedings of the National Academy of Sciences of the United States of America·A A Danen-Van OorschotM H Noteborn
Aug 5, 2009·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Menno J OudhoffEnno C I Veerman
Mar 1, 1996·Archives of Dermatological Research·M SerresD Schmitt
Mar 1, 1987·Clinical and Experimental Dermatology·K Smith, S Shuster
Jul 1, 1984·The British Journal of Dermatology·M Prunieras, C Delescluse
Mar 1, 1982·The British Journal of Dermatology·A Hughes, H J Yardley
Jun 8, 2007·The British Journal of Dermatology·Q le DucS Gibbs
Sep 24, 2004·Physiological Reviews·Andrzej SlominskiJacobo Wortsman
May 23, 2018·Drug Testing and Analysis·Victor CarrerLuisa Coderch
Jan 1, 1985·Archives of Dermatological Research·A Ohkawara, H Iizuka
Jun 1, 1988·International Journal of Dermatology·J Fransson, H Hammar
Jul 14, 1999·Archives of Pharmacal Research·H J Lee, D H Ko
Jul 8, 2000·Wound Repair and Regeneration : Official Publication of the Wound Healing Society [and] the European Tissue Repair Society·S GibbsM Ponec
Sep 1, 2019·International Journal of Molecular Sciences·Deborah MinzaghiSandrine Dubrac
Aug 1, 1988·In Vitro Cellular & Developmental Biology : Journal of the Tissue Culture Association·M PonecJ Boonstra
Jan 1, 1983·Archives of Dermatological Research·M Ponec, J A Kempenaar
Nov 28, 2008·Chemical Reviews·M Omar F Khan, Henry J Lee
May 1, 1988·Molecular and Cellular Biology·T KartasovaP van de Putte
Aug 1, 1983·The Journal of Investigative Dermatology·M PonecB J Vermeer
Dec 1, 1984·The Journal of Investigative Dermatology·M PonecB J Vermeer
Jun 1, 1983·The Journal of Investigative Dermatology·H Iizuka, A Ohkawara
Oct 1, 1983·The Journal of Investigative Dermatology·K M LeifermanT C Spelsberg
Feb 1, 1982·The Journal of Investigative Dermatology·E H Epstein, J M Bonifas
Sep 1, 1997·The Journal of Investigative Dermatology·M PonecA M Mommaas

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