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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.