Definition of the critical cellular components which distinguish between hormone and antihormone activated progesterone receptor

The steroid hormone progesterone is a key modulator of the cellular processes associated with the maintenance and development of female reproductive function. The biological activity of this hormone is mediated by specific nuclear receptors located in target cell nuclei which upon activation are cap...

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Bibliographic Details
Published in:Journal of steroid biochemistry and molecular biology 1995-06, Vol.53 (1), p.487-495
Main Authors: Clemm, David L., Macy, Bryan L., Santiso-Mere, Dolores, McDonnell, Donald P.
Format: Article
Language:English
Subjects:
Biological and medical sciences
DNA-Binding Proteins - physiology
Gene Expression Regulation
Hormones. Endocrine system
Humans
Macromolecular Substances
Medical sciences
Mifepristone - analogs & derivatives
Mifepristone - pharmacology
Pharmacology. Drug treatments
Progesterone - chemistry
Promoter Regions, Genetic
Receptors, Progesterone - antagonists & inhibitors
Receptors, Progesterone - classification
Receptors, Progesterone - physiology
Receptors, Steroid - physiology
Repressor Proteins
Signal Transduction
Structure-Activity Relationship
Transcription, Genetic
Transcriptional Activation
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Summary:The steroid hormone progesterone is a key modulator of the cellular processes associated with the maintenance and development of female reproductive function. The biological activity of this hormone is mediated by specific nuclear receptors located in target cell nuclei which upon activation are capable of modulating the transcriptional activity of promoters containing progesterone response elements. Abnormalities in the progesterone receptor (PR) signal transduction pathway are implicated in pathological states such as breast cancer, endometriosis, and uterine fibroids. As a result of the medical need to modulate PR transcriptional activity, antiprogestins, compounds which oppose the actions of progesterone and novel progesterone receptor agonists, have been developed. This review outlines our current understanding of the critical cellular components which define the pharmacology of progesterone receptor agonists and antagonists, and how this information will impact the discovery and development of additional therapeutics.
ISSN:0960-0760
1879-1220
DOI:10.1016/0960-0760(95)00095-H