Document Detail

Effects of bicalutamide and 4OH-tamoxifen on androgen-regulated gene expression in the LNCaP cell line.
MedLine Citation:
PMID:  23225433     Owner:  NLM     Status:  MEDLINE    
BACKGROUND: Bicalutamide (BIC) is an alternative treatment to castration for advanced prostate cancer. Breast events are common adverse effects which can be effectively prevented by the concurrent administration of tamoxifen, a selective estrogen receptor modulator.
MATERIALS AND METHODS: We investigated the effects of BIC, 4-hydroxy Tamoxifen (4OHT), the active metabolite of tamoxifen, and their combination on the expression of a panel of genes implicated in prostate cancer development and progression in LNCaP cells stimulated with dihydrotestosterone.
RESULTS: Our findings confirm the anti-proliferative activity of BIC on LNCaP cell growth but also show the down-regulating function of this anti-androgen on the expression of genes involved in tumor proliferation and invasion [cyclins, caspases, epidermal growth factor (EGF)]. The combination with 4OHT exerts a synergistic effect on the downregulation of some genes involved in prostate cancer progression.
CONCLUSION: The observation that the expression of several genes [such as B-cell lymphoma-2 (BCL2), myelocytomatosis oncogene (MYC), caspases] is modulated midly-to-moderately, after 4OHT addition suggests that this combined approach in the clinical setting should be further investigated through appropriate trials.
Rosa Mangerini; Francesca Argellati; Ulrich Pfeffer; Francesco Boccardo
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Anticancer research     Volume:  32     ISSN:  1791-7530     ISO Abbreviation:  Anticancer Res.     Publication Date:  2012 Dec 
Date Detail:
Created Date:  2012-12-10     Completed Date:  2013-05-02     Revised Date:  2013-05-27    
Medline Journal Info:
Nlm Unique ID:  8102988     Medline TA:  Anticancer Res     Country:  Greece    
Other Details:
Languages:  eng     Pagination:  5323-9     Citation Subset:  IM    
Department of Medical Oncology, IRCCS SAN Martino Hospital - IST National Cancer Research Institute, Largo R. Benzi 10, 16132 Genoa, Italy.
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MeSH Terms
Androgens / physiology*
Anilides / administration & dosage,  pharmacology*
Antineoplastic Combined Chemotherapy Protocols / pharmacology*
Cell Growth Processes / drug effects,  genetics
Cell Line, Tumor
Gene Expression Regulation, Neoplastic / drug effects*
Kallikreins / biosynthesis
Neoplasms, Hormone-Dependent / drug therapy,  genetics
Nitriles / administration & dosage,  pharmacology*
Prostate-Specific Antigen / biosynthesis
Prostatic Neoplasms / drug therapy*,  genetics*
Tamoxifen / administration & dosage,  analogs & derivatives*,  pharmacology
Tosyl Compounds / administration & dosage,  pharmacology*
Reg. No./Substance:
0/Androgens; 0/Anilides; 0/Nitriles; 0/Tosyl Compounds; 10540-29-1/Tamoxifen; 17197F0KYM/afimoxifene; 90357-06-5/bicalutamide; EC 3.4.21.-/Kallikreins; EC 3.4.21.-/kallikrein-related peptidase 3, human; EC Antigen

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