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Definition of the molecular and cellular mechanisms underlying the tissue-selective agonist/antagonist activities of selective estrogen receptor modulators.

Publication ,  Journal Article
McDonnell, DP; Connor, CE; Wijayaratne, A; Chang, C-Y; Norris, JD
Published in: Recent Prog Horm Res
2002

The term selective estrogen receptor modulators describes a group of pharmaceuticals that function as estrogen receptor (ER) agonists in some tissues but that oppose estrogen action in others. Although the name for this class of drugs has been adopted only recently, the concept is not new, as compounds exhibiting tissue-selective ER agonist/antagonist properties have been around for nearly 40 years. What is new is the idea that it may be possible to capitalize on the paradoxical activities of these drugs and develop them as target organ-selective ER agonists for the treatment of osteoporosis and other estrogenopathies. This realization has provided the impetus for research in this area, the progress of which is discussed in this review.

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Published In

Recent Prog Horm Res

DOI

ISSN

0079-9963

Publication Date

2002

Volume

57

Start / End Page

295 / 316

Location

United States

Related Subject Headings

  • Tamoxifen
  • Structure-Activity Relationship
  • Selective Estrogen Receptor Modulators
  • Receptors, Estrogen
  • Protein Conformation
  • Humans
  • Female
  • Estrogen Receptor beta
  • Estrogen Antagonists
  • Endocrinology & Metabolism
 

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McDonnell, D. P., Connor, C. E., Wijayaratne, A., Chang, C.-Y., & Norris, J. D. (2002). Definition of the molecular and cellular mechanisms underlying the tissue-selective agonist/antagonist activities of selective estrogen receptor modulators. Recent Prog Horm Res, 57, 295–316. https://doi.org/10.1210/rp.57.1.295
McDonnell, Donald P., Caroline E. Connor, Ashini Wijayaratne, Ching-Yi Chang, and John D. Norris. “Definition of the molecular and cellular mechanisms underlying the tissue-selective agonist/antagonist activities of selective estrogen receptor modulators.Recent Prog Horm Res 57 (2002): 295–316. https://doi.org/10.1210/rp.57.1.295.
McDonnell, Donald P., et al. “Definition of the molecular and cellular mechanisms underlying the tissue-selective agonist/antagonist activities of selective estrogen receptor modulators.Recent Prog Horm Res, vol. 57, 2002, pp. 295–316. Pubmed, doi:10.1210/rp.57.1.295.

Published In

Recent Prog Horm Res

DOI

ISSN

0079-9963

Publication Date

2002

Volume

57

Start / End Page

295 / 316

Location

United States

Related Subject Headings

  • Tamoxifen
  • Structure-Activity Relationship
  • Selective Estrogen Receptor Modulators
  • Receptors, Estrogen
  • Protein Conformation
  • Humans
  • Female
  • Estrogen Receptor beta
  • Estrogen Antagonists
  • Endocrinology & Metabolism