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differentiation of male urogenital structures (male external genitalia, urethra, and prostate; Wilson et al . 1993 , Nef & Parada 2000 ). To mediate their actions, testosterone, and DHT bind to the intracellular androgen receptor (AR), a ligand
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placenta are associated with complications such as preeclampsia and preterm delivery ( Albrecht & Pepe 2010 ). Estrogen acts by binding to its receptor, estrogen receptor (ER). ER exists in two main forms, ERα (ESR1) and ERβ (ESR2), which have distinct
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The nuclear receptor family comprises ligand-dependent and orphan receptors. To the latter group belong the estrogen receptor-related receptors (ERRs) for which conflicting results have been published concerning the nature (constitutive or liganded) of their transcriptional activities. ERRs interfere in various ways, positively and negatively, with estrogen signaling. Moreover recent data analyzing ERR expression in human breast tumors have proposed ERRalpha and ERRgamma as prognostic markers of these cancers. The identification of modulators (positive or negative) of ERR activities would therefore be highly useful in our understanding of estrogen-related pathologies. The purpose of this review is to summarize our knowledge of the nature of ERR activities and progresses in identifying synthetic ERR modulators.
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Introduction The opioid receptor-like (ORL1; also called NOP) receptor is a G-protein-coupled receptor (GPCR) that shares high sequence identity with the three classically recognized opioid receptor types, μ, δ, and κ ( Mollereau et
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system ( Gomariz et al. 2001 ). The effects of VIP are mediated through interaction with two receptor subclasses named VPAC 1 and VPAC 2 receptors ( Harmar et al. 1998 ). These receptors are members of the G-protein-coupled receptor (GPCR)-B family
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Introduction Kappa (κ), delta (δ), mu (μ) and ORL1 (opioid receptor-like) represent the four main classes of opioid receptors, which are defined and distinguished by primary structures, anatomical distributions, pharmacological
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Introduction The melanocortin-4 receptor (MC4R) is encoded by a single-exon gene and is primarily expressed in the hypothalamic paraventricular nucleus, spinal cord, sympathetic preganglionic neurons, brain stem, and penis ( Van der Ploeg et al
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Historical perspective Nuclear receptors are a large family of DNA-binding transcription factors that are recruited to specific DNA sequences in the genome and regulate the expression of genes in the proximity (<1 million base pairs) of these sites
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Introduction Nuclear receptors (NRs) are essential to animal life, but their evolutionary origins are unknown. NRs are present in Metazoan species including sponges, insects, and vertebrates, but not in Archaea, bacteria, fungi, or plants. NRs
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Introduction G protein-coupled receptors (GPCRs) constitute the major family of cell surface receptors. They comprise receptors for light, taste, and smell as well as receptors for ions, small transmitters, peptides, and large protein hormones
