Androgen Receptor (AR)
The androgen receptor (AR) is a member of the steroidhormone family of receptors, together with the estrogen, progesterone, and glucocorticoid receptors.The androgen receptor is one of the 49 members of the steroid receptor family of ligand-activated transcription factors.The steroid or nuclear hormone receptors play pivotal roles in the organogenesis, physiology, and pathology of a variety of tissues. These receptors are promiscuously activated by wide-ranging ligands, including natural hormones, growth factors, peptides, or synthetic molecules. The steroid receptor family is organized into three classes. Class I is comprised of receptors for hormones such as androgens, progestins, estrogens, and corticosteroids. Receptors for vitamins and thyroid hormones belong to class II, while receptors for bile acids and for which natural ligands have not yet been identified are relegated to class III.The discovery of selective androgen receptor modulators (SARMs) and other tissue-selective nuclear hormone receptor modulators that activate their cognate receptors in a tissue-selective manner provides an opportunity to promote the beneficial effects of androgens and other hormones in target tissues with greatly reduced unwanted side-effects.SARMs have been proposed as treatments of choice for various diseases, including muscle-wasting, breast cancer, and osteoporosis.
References
1.Gucalp A,et al. Ann Surg Oncol. 2017 Oct;24(10):2876-2880.
2.Ramesh Narayanan,et al. Mol Cell Endocrinol. 2018 Apr 15; 465: 134–142.
References
1.Gucalp A,et al. Ann Surg Oncol. 2017 Oct;24(10):2876-2880.
2.Ramesh Narayanan,et al. Mol Cell Endocrinol. 2018 Apr 15; 465: 134–142.
Endocrinology/Hormones
Androgen Receptor (AR)
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BMS-986365
catalog no : M37509
cas no: 2446928-30-7
BMS-986365 (CC-94676) is an orally available, selective and highly potent AR degrader with potential anticancer activity that inhibits AR signaling and suppresses tumor growth for the study of prostate cancer. -
Zanoterone
catalog no : M36136
cas no: 107000-34-0
Zanoterone is an AR antagonist (androgen receptor).Zanoterone has antitumor activity for the treatment of genitourinary disorders and oncological disorders and may be used in the study of prostate cancer. -
BMS-641988 B
catalog no : M36006
cas no: 1093276-09-5
BMS-641988 is a novel nonsteroidal androgen receptor antagonist for the treatment of prostate cancer. -
Rezvilutamide
catalog no : M35089
cas no: 1572045-62-5
Rezvilutamide (SHR3680) is an orally available androgen receptor inhibitor that crosses the blood-brain barrier and has antitumor activity.Rezvilutamide (SHR3680) is used in the study of metastatic desmoplasia-resistant prostate cancer. -
Ralaniten triacetate
catalog no : M34834
cas no: 1637573-04-6
Ralaniten triacetate (EPI-506), a precursor of Ralaniten, is a first-of-its-kind, orally active androgen receptor N-terminal structural domain (AR-NTD) inhibitor with anticancer activity and can be used to study prostate and breast cancer.