Library Subscription: Guest
Begell Digital Portal Begell Digital Library eBooks Journals References & Proceedings Research Collections
Critical Reviews™ in Eukaryotic Gene Expression
IF: 1.841 5-Year IF: 1.927 SJR: 0.649 SNIP: 0.516 CiteScore™: 1.96

ISSN Print: 1045-4403
ISSN Online: 2162-6502

Critical Reviews™ in Eukaryotic Gene Expression

DOI: 10.1615/CritRevEukarGeneExpr.v20.i4.10
pages 275-294

Modulators of Androgen and Estrogen Receptor Activity

Bart L. Clarke
Mayo Clinic, Rochester, Minnesota, USA
Sundeep Khosla
Mayo Clinic Endocrine Research Unit, Rochester, Minnesota, USA

ABSTRACT

This review focuses on significant recent findings regarding modulators of androgen and estrogen receptor activity. Selective androgen receptor modulators (SARMs) interact with androgen receptors (ARs), and selective estrogen receptor modulators (SERMs) interact with estrogen receptors (ERs), with variable tissue selectivity. SERMs, which interact with both ERб and ERв in a tissue-specific manner to produce diverse outcomes in multiple tissues, continue to generate significant interest for clinical application. Development of SARMs for clinical application has been slower to date because of potential adverse effects, but these diverse compounds continue to be investigated for use in disorders in which modulation of the AR is important. SARMs have been investigated mostly at the basic and preclinical level to date, with few human clinical trials published. These compounds have been evaluated mostly for application in different stages of prostate cancer to date, but they hold promise for multiple other applications. Publication of the large STAR and RUTH clinical trials demonstrated that the SERMs tamoxifen and raloxifene have interesting similarities and differences in tissues that contain ERs. Lasofoxifene, bazedoxifene, and arzoxifene are newer SERMs that have been demonstrated in clinical trials to more potently increase bone mineral density and lower serum cholesterol values than tamoxifen or raloxifene. Both SARMs and SERMs hold great promise for therapeutic use in multiple disorders in which tissue-specific effects are mediated by their respective receptors.


Articles with similar content:

Drug Delivery to the Nail: Therapeutic Options and Challenges for Onychomycosis
Critical Reviews™ in Therapeutic Drug Carrier Systems, Vol.31, 2014, issue 6
Bhavesh S. Barot, Pragna K. Shelat, Hetal K. Patel, Dharmik M. Mehta, Punit B. Parejiya
Biodegradable Microspheres in Drug Delivery
Critical Reviews™ in Therapeutic Drug Carrier Systems, Vol.12, 1995, issue 1
Hajime Toguchi, Hiroaki Okada
Oral Delivery of HIV-Protease Inhibitors
Critical Reviews™ in Therapeutic Drug Carrier Systems, Vol.17, 2000, issue 2
Barbra H. Stewart, Lilian Y. Li, David Fleisher
Steroid Receptors as Molecular Targets for Cancer Diagnosis and Therapy
Critical Reviews™ in Therapeutic Drug Carrier Systems, Vol.26, 2009, issue 3
Vandana Soni, Piush Khare, Suresh P. Vyas, Aviral Jain, Arvind Gulbake, Sanjay Kumar Jain, Pramod Mishra
Photodynamic Therapy and Detection of High-Grade Gliomas
Journal of Environmental Pathology, Toxicology and Oncology, Vol.25, 2006, issue 1-2
Henry Hirschberg, Steen J. Madsen