Targeting the Androgen Receptor with Steroid Conjugates
نویسندگان
چکیده
منابع مشابه
Targeting the Androgen Receptor with Steroid Conjugates
The androgen receptor (AR) is a major therapeutic target in prostate cancer pharmacology. Progression of prostate cancer has been linked to elevated expression of AR in malignant tissue, suggesting that AR plays a central role in prostate cancer cell biology. Potent therapeutic agents can be precisely crafted to specifically target AR, potentially averting systemic toxicities associated with no...
متن کاملCharacterizing and Targeting Androgen Receptor
The androgen receptor (AR) is the principal therapeutic target in prostate cancer. For the past 70 years, androgendeprivation therapy (ADT) has been the major therapeutic focus. However, some patients do not benefit, and those tumorsthat do initially respond to ADT eventually progress. One recently described mechanism of such an effect is growth andsurvival-promoting effects of the ...
متن کاملThe Evolution of Prostate Cancer Therapy: Targeting the Androgen Receptor
Prostate cancer treatment has evolved through the varying eras of therapy from one of predominantly hormonal agents without much effective cytotoxic therapy until the use of docetaxel was found to improve overall survival in the pivotal TAX-327 (1) and SWOG 99-16 trials (2). While efforts to search for the appropriate docetaxel partner has yielded disappointing results with multiple Phase III t...
متن کاملTargeting androgen receptor in estrogen receptor-negative breast cancer.
Endocrine therapies for breast cancer that target the estrogen receptor (ER) are ineffective in the 25%-30% of cases that are ER negative (ER-). Androgen receptor (AR) is expressed in 60%-70% of breast tumors, independent of ER status. How androgens and AR regulate breast cancer growth remains largely unknown. We find that AR is enriched in ER- breast tumors that overexpress HER2. Through analy...
متن کاملP-202: StuI Polymorphism on the Androgen Receptor Gene in Women with Endometriosis
Background: Androgens have an anti-proliferative effect on endometrial cells. Human androgen receptor (AR) gene contains two polymorphic short tandem repeats of GGC and CAG, and a single-nucleotide polymorphism on exon 1 that is recognized by the restriction enzyme, StuI. Prior studies have shown that the lengths of the CAG and GGC repeats are inversely and linearly related to AR activity and a...
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ژورنال
عنوان ژورنال: Journal of Medicinal Chemistry
سال: 2014
ISSN: 0022-2623,1520-4804
DOI: 10.1021/jm500101h