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ORG-2058 as a ligand in the assay of progesterone receptor in breast cancer.

Abstract
Tritiated [(16 alpha-ethyl-21-hydroxy-19-nor-pregn-4-ene-3,20-dione)-6,7-3H] (ORG-2058) and 17,21-dimethyl-19-nor-pregna-4,9-diene-3,20-dione (R5020) were compared as ligands in the assay of progesterone receptor in human and rat breast tumors. We found that ORG-2058 is a better ligand because of its low nonspecific binding. Most of the nonspecific binding of the other ligand R5020, is to proteins which bind corticosteroids. In cancerous tissue ORG-2058 binds to progesterone receptor linearly in a range of protein concentrations which are normally used in the receptor assay. On the other hand, R5020 exhibits binding linearity over a narrower protein concentration in many tumor biopsies, which may cause severe limitation in the assay procedure or frequent underestimation of receptor content.
AuthorsY Sharoni, B Feldman, N Karny, J Levy
JournalSteroids (Steroids) 1986 Nov-Dec Vol. 48 Issue 5-6 Pg. 419-26 ISSN: 0039-128X [Print] United States
PMID3445291 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Pregnenediones
  • Receptors, Progesterone
  • 16 alpha-ethyl-21-hydroxy-19-nor-4-pregnene-3,20-dione
  • Promegestone
Topics
  • Animals
  • Breast Neoplasms (metabolism)
  • Cytosol (metabolism)
  • Female
  • Humans
  • Male
  • Mammary Neoplasms, Experimental (metabolism)
  • Pregnenediones
  • Promegestone
  • Rats
  • Receptors, Progesterone (analysis)
  • Uterus (metabolism)

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