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Orphan Nuclear Receptor Modulators

Current Topics in Medicinal Chemistry, 2003
Nuclear hormone receptors are ligand-activated transcription factors that regulate gene expression and play a critical role in endocrine signaling. Orphan nuclear receptors belong to this gene super-family but their target genes and physiological function have not been completely elucidated.
Raju, Mohan, Richard A, Heyman
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Orphan nuclear receptors adopted by crystallography

Current Opinion in Structural Biology, 2005
Of the large nuclear hormone receptor superfamily of proteins, orphan nuclear receptors have remained a mystery owing to their lack of identified ligands and their constitutive nature. Now, structures of several ligand-binding domains of orphan receptors have provided some surprising insights that were not anticipated from molecular studies. Therefore,
Holly A, Ingraham, Matthew R, Redinbo
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Orphan Nuclear Receptors

2000
The nuclear receptor superfamily consists of a class of transcription factors comprising more than 100 different proteins. In contrast to membrane-bound receptors, the nuclear receptors are intracellular and act by controlling the activity of genes directly. Most members of this family bind directly to small lipidsoluble signaling molecules, or ligands,
Deepak S. Lala, Richard A. Heyman
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Gene Silencing by Nuclear Orphan Receptors

2004
Nuclear orphan receptors represent a large and diverse subgroup in the nuclear receptor superfamily. Although putative ligands for these orphan members remain to be identified, some of these receptors possess intrinsic activating, inhibitory, or dual regulatory functions in development, differentiation, homeostasis, and reproduction.
Ying, Zhang, Maria L, Dufau
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Orphan Nuclear Receptors: Shifting Endocrinology into Reverse

Science, 1999
Steroid and thyroid hormones and vitamin A metabolites (retinoids) regulate the expression of complex gene programs by binding to members of the nuclear receptor family of ligand-activated transcription factors. The nuclear receptor family also includes many “orphan” members that currently lack known ligands but that represent candidate receptors for ...
S A, Kliewer, J M, Lehmann, T M, Willson
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The mammalian orphan nuclear receptors: orphans as cellular guardians

Journal of Receptors and Signal Transduction, 2010
In classical endocrinology, receptors are molecules that bind a hormone or a ligand to transduce signal within a target cell. Later, however, many intracellular receptors have been discovered in mammals, which have not been shown to bind endogenous ligands and are now are referred as "orphan receptors." The orphan receptors share high degree of ...
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Chemical Genomics of Orphan Nuclear Receptors

2003
The steroid hormone, thyroid hormone, retinoic acid, and vitamin D receptors are members of a family of ligand-activated transcription factors (Mangelsdorf et al. 1995). These nuclear hormone receptors contain two signature domains, a central double zinc finger DNA-binding domain (DBD) and a C-terminal ligand-binding domain (LBD) (Fig. 1).
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Orphan nuclear receptors: therapeutic opportunities in skeletal muscle

American Journal of Physiology-Cell Physiology, 2006
Nuclear hormone receptors (NRs) are ligand-dependent transcription factors that bind DNA and translate physiological signals into gene regulation. The therapeutic utility of NRs is underscored by the diversity of drugs created to manage dysfunctional hormone signaling in the context of reproductive biology, inflammation, dermatology, cancer, and ...
Smith, Aaron G., Muscat, George E. O.
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