Literature DB >> 11108892

Progesterone receptor modulators and progesterone antagonists in women's health.

I M Spitz1, K Chwalisz.   

Abstract

Both progesterone receptor modulators (PRMs) as well as pure progesterone antagonists (PAs) have numerous proven and potential therapeutic applications in female health care. Mifepristone, a PRM with only marginal agonistic activity, together with a prostaglandin can terminate pregnancies of less than 9 weeks duration; mifepristone is also used in the preparation of women at later gestational stages whose pregnancies are terminated with prostaglandins or surgery. Mifepristone causes expulsion of the uterine contents following intrauterine fetal death and promotes dilation of the non-pregnant primigravid uterus. It is also effective in the treatment of missed abortion. Together with methotrexate, mifepristone can be used in the medical treatment of ectopic pregnancy. Both PAs and PRMs display antiproliferative effects on the endometrium. Because of this, they have application in the treatment of endometriosis, an estrogen-dependent condition. They may also be utilized to reduce myoma size, acting as both a PA and antiproliferative agent. Unlike GnRH agonists, long-term use in endometriosis and myoma is not associated with loss of bone and hypoestrogenism. PRMs may also be useful in IVF programs to prevent a premature LH surge and to delay the emergence of the implantation window. Some PRMs have potential use as hormone replacement therapy in women during menopause or in those with dysfunctional uterine bleeding.

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Year:  2000        PMID: 11108892     DOI: 10.1016/s0039-128x(00)00194-x

Source DB:  PubMed          Journal:  Steroids        ISSN: 0039-128X            Impact factor:   2.668


  11 in total

Review 1.  Proven and potential clinical applications of mifpristone (RU486).

Authors:  Irving M Spitz
Journal:  Rev Endocr Metab Disord       Date:  2002-09       Impact factor: 6.514

2.  X-ray structures of progesterone receptor ligand binding domain in its agonist state reveal differing mechanisms for mixed profiles of 11β-substituted steroids.

Authors:  Scott J Lusher; Hans C A Raaijmakers; Diep Vu-Pham; Bert Kazemier; Rolien Bosch; Ross McGuire; Rita Azevedo; Hans Hamersma; Koen Dechering; Arthur Oubrie; Marcel van Duin; Jacob de Vlieg
Journal:  J Biol Chem       Date:  2012-04-25       Impact factor: 5.157

3.  Structural basis for agonism and antagonism for a set of chemically related progesterone receptor modulators.

Authors:  Scott J Lusher; Hans C A Raaijmakers; Diep Vu-Pham; Koen Dechering; Tsang Wai Lam; Angus R Brown; Niall M Hamilton; Olaf Nimz; Rolien Bosch; Ross McGuire; Arthur Oubrie; Jacob de Vlieg
Journal:  J Biol Chem       Date:  2011-08-17       Impact factor: 5.157

Review 4.  Role of nuclear progesterone receptor isoforms in uterine pathophysiology.

Authors:  Bansari Patel; Sonia Elguero; Suruchi Thakore; Wissam Dahoud; Mohamed Bedaiwy; Sam Mesiano
Journal:  Hum Reprod Update       Date:  2014-11-18       Impact factor: 15.610

5.  Coactivator/corepressor ratios modulate PR-mediated transcription by the selective receptor modulator RU486.

Authors:  Zheng Liu; Didier Auboeuf; Jiemin Wong; J Don Chen; Sophia Y Tsai; Ming-Jer Tsai; Bert W O'Malley
Journal:  Proc Natl Acad Sci U S A       Date:  2002-06-04       Impact factor: 11.205

6.  The selective progesterone receptor modulator CDB4124 inhibits proliferation and induces apoptosis in uterine leiomyoma cells.

Authors:  Xia Luo; Ping Yin; John S Coon V; You-Hong Cheng; Ronald D Wiehle; Serdar E Bulun
Journal:  Fertil Steril       Date:  2010-01-08       Impact factor: 7.329

7.  Demonstration of mixed properties of RU486 in progesterone receptor (PR)-transfected MDA-MB-231 cells: a model for studying the functions of progesterone analogues.

Authors:  V C Lin; S E Aw; E H Ng; E H Ng; M G Tan
Journal:  Br J Cancer       Date:  2001-12-14       Impact factor: 7.640

8.  Uterine fibroids may play a protecting role against endometrial carcinoma in Chinese women with gynecological diseases.

Authors:  Li Qiao; Lili Xia; Yan Dong; Yajuan Cheng; Hongbao Cao
Journal:  Biosci Rep       Date:  2020-07-31       Impact factor: 3.840

9.  Safety, efficacy and patient satisfaction with continuous daily administration of levonorgestrel/ethinylestradiol oral contraceptives.

Authors:  Giuseppe Benagiano; Sabina Carrara; Valentina Filippi
Journal:  Patient Prefer Adherence       Date:  2009-11-03       Impact factor: 2.711

Review 10.  Abnormal bleeding during menopause hormone therapy: insights for clinical management.

Authors:  Sebastião Freitas de Medeiros; Márcia Marly Winck Yamamoto; Jacklyne Silva Barbosa
Journal:  Clin Med Insights Womens Health       Date:  2013-01-23
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