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Targeting the Estrogen Receptor using Steroid-Therapeutic Drug Conjugates.
MedLine Citation:
PMID:  23036054     Owner:  NLM     Status:  Publisher    
Abstract: The estrogen receptor (ER) is a potentially useful biological target for the diagnosis and therapy in hormonally responsive human breast cancer. This protein is often over expressed both on the membrane and nuclear compartment of breast cancer cells and provides a mechanism for both localization and therapy. Over the past 30 years many research groups have attempted to exploit the high affinity and receptor selectivity of steroidal estrogens to deliver cytotoxic agents that by themselves lack selectivity. In this review we describe the strategies and methods employed by those investigators in their efforts to develop steroid-drug conjugates the goals of enhanced antiproliferative activity and ER-selectivity. In particular, the choices of steroid scaffolds and sites for drug conjugation have evolved as the understanding of role of ER in cell function has expanded. Present knowledge of the mechanism of action for estrogens and antiestrogens helps explain the failure of most efforts to achieve their stated objectives. The review culminates in the description of our program which has produced the first conjugate that clearly has achieved those goals and provides an approach for developing new agents for future clinical use.
Kinh-Luan D Dao; Robert N Hanson
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-10-5
Journal Detail:
Title:  Bioconjugate chemistry     Volume:  -     ISSN:  1520-4812     ISO Abbreviation:  Bioconjug. Chem.     Publication Date:  2012 Oct 
Date Detail:
Created Date:  2012-10-5     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9010319     Medline TA:  Bioconjug Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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