Editorial [Hot Topic: Nuclear Receptors as Targets in Drug Discovery: Medicinal Chemistry and Therapeutic Potential (Guest Editor: Mary J. Meegan)]

摘要

Nuclear receptors have become an important focus of clinical and pharmaceutical investigation as they represent targets for many of the key lipophilic hormones such as steroids, thyroxine and retinoic acid. These receptors include the Androgen Receptor (AR), Estrogen Receptor (ER), Progesterone Receptor (PR), Glucocorticoid receptor (GR), Peroxisome Proliferator-Activated Receptor (PPAR), Thyroid Receptor (TR), Vitamin D Receptor and the various Steroid Receptor associated proteins (SRAPR). These receptors function as ligand dependent transcriptional regulators and are involved in the regulation of many critical biochemical processes such as cell differentiation, development and proliferation. The understanding of the complex chemical structure and biochemical function of the nuclear receptor family has expanded considerably in recent years in the areas of hormonal signal transduction pathways and elucidation of the molecular mechanisms by which gene activity is directly regulated by the hormone receptor complex. The review topics highlight the central role of the estrogen receptor (ER) as a target in breast cancer including the development of acquired resistance to exhaustive use of endocrine therapy and the mechanism of endocrine based therapy resistance. The Estrogen-related Receptors (ERR) are now recognized as potential therapeutic targets and clinical markers in breast cancer.