International Union of Pharmacology. LXV. The Pharmacology and Classification of the Nuclear Receptor Superfamily: Glucocorticoid, Mineralocorticoid, Progesterone, and Androgen Receptors

  title={International Union of Pharmacology. LXV. The Pharmacology and Classification of the Nuclear Receptor Superfamily: Glucocorticoid, Mineralocorticoid, Progesterone, and Androgen Receptors},
  author={Nick Z Lu and Suzanne E. Wardell and Kerry L. Burnstein and Donald B. DeFranco and Peter J. Fuller and Vincent Gigu{\`e}re and Richard B. Hochberg and Lorraine Mckay and Jack Michel Renoir and Nancy L. Weigel and Elizabeth M. Wilson and Donald P. McDonnell and John A. Cidlowski},
  journal={Pharmacological Reviews},
  pages={782 - 797}
The glucocorticoid receptor (GR[1][1]), mineralocorticoid receptor (MR), progesterone receptor (PR), and androgen receptor (AR) are classic members of the nuclear receptor superfamily, composing subfamily 3C. Members of this subfamily are among those receptors that were cloned the earliest, with the 
Differential interactions of antiretroviral agents with LXR, ER and GR nuclear receptors: potential contributing factors to adverse events
The closely related liver X receptors, oestrogen receptors and glucocorticoid receptor regulate many endogenous processes such as lipid/cholesterol homeostasis, cellular differentiation and inflammation.
Steroidal Mineralocorticoid Receptor Antagonists: Synthesis and Biology
The development of selective steroidal mineralocorticoid receptor antagonists with improved pharmacological profiles over existing marketed drugs is an attractive goal and new spirolactones 11 and 20 were identified with promising biological profiles.
Nuclear Hormone Receptor Medicinal Chemistry
This chapter will be focused on recent advances in the medicinal chemistry of agonist, antagonist, and modulator ligands of selected nuclear hormone receptors (NHRs) that are of special interest in
Tissue-specific glucocorticoid action: a family affair
Opportunities for development of novel therapies targeting steroid hormone receptors
Opportunities and challenges in the development of novel therapeutic agents targeting members of the steroid hormone receptors are discussed.
Met909 Plays a Key Role in the Activation of the Progesterone Receptor and Also in the High Potency of 13-Ethyl Progestins
The crystal structure of the ligand-binding domain of the human PR complexed with levonorgestrel, a potent testosterone-derived progestin characterized by a 13-ethyl substituent, is solved and provides a structural guideline for the rational synthesis of potent PR agonist and antagonist ligands that could have therapeutic uses in women's health.
Structures of androgen receptor bound with ligands: advancing understanding of biological functions and drug discovery
The structures of AR-ligand complexes are an invaluable scientific asset that enhances the understanding of biological functions and mechanisms of androgenic and anti-androgenic chemicals as well as promotes the discovery of superior drug candidates.
Selective androgen receptor modulators in preclinical and clinical development
This review summarizes the current standing of research and development of Selective androgen receptor modulators, crystallography of AR with SARMs, plausible mechanisms for their action and the potential therapeutic indications for this emerging class of drugs.
Evidence to Support The Non-Genomic Modulation of The HPA Axis
The evidence supporting a role for non-genomic effects of the stress hormone corticosterone in the body’s response to stress is reviewed.


The glucocorticoid receptor beta-isoform: a perspective on its relevance in human health and disease.
S steroid hormones that are secreted by the adrenal gland in a diurnal rhythm and after acute stress are used to treat a wide variety of diseases, including allergic and autoimmune diseases like asthma and rheumatoid arthritis.
Study of androgen receptor functions by genetic models.
Recent results of studies into genetic models of the loss of AR function in mice and the gain of ARfunction in Drosophila are reviewed.
Atomic structure of progesterone complexed with its receptor
The 1.8 Å crystal structure of a progesterone-bound ligand-binding domain of the human progester one receptor is reported, which explains the receptor's selective affinity for progestins and establishes a common mode of recognition of 3-oxy steroids by the cognate receptors.
  • P. Pearce, J. Funder
  • Biology, Medicine
    Clinical and experimental pharmacology & physiology
  • 1987
1. The use of the receptor stabilizing agent sodium molybdate, and of RU26988 to exclude [3H]‐aldosterone binding from Type II glucocorticoid receptors, has enabled the characterization of high
Multiple aspects of mineralocorticoid selectivity.
Several cellular and molecular mechanisms intervene to allow specific aldosterone regulatory effects, despite the large prevalence of glucocorticoid hormones in the plasma.
Molecular mechanisms of mineralocorticoid receptor antagonism by eplerenone.
The preclinical and clinical evidence supporting the beneficial effects of eplerenone (INSPRA), a selective aldosterone blocker, in the treatment of hypertension and heart failure is summarized and the current status in understanding the molecular mechanisms of action of the MR and its ligand is reviewed.