The Concise Guide to PHARMACOLOGY 2015/16:Nuclear hormone receptors [PDF]
The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org),
Aldrich, R +151 more
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The therapeutic potential of RORγ modulators in the treatment of human disease
Mi Ra Chang,1 Devrishi Goswami,1 Becky A Mercer,2 Patrick R Griffin1,21Department of Molecular Therapeutics, Scripps Florida, The Scripps Research Institute, Jupiter, FL, USA; 2Translational Research Institute, Scripps Florida, The Scripps Research ...
Chang MR +3 more
doaj
The human orphan nuclear receptor tailless (TLX, NR2E1) is druggable. [PDF]
Nuclear receptors (NRs) are an important group of ligand-dependent transcriptional factors. Presently, no natural or synthetic ligand has been identified for a large group of orphan NRs.
Cindy Benod +9 more
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Direct genetic demonstration of Gα13 coupling to the orphan G protein-coupled receptor G2A leading to RhoA-dependent actin rearrangement [PDF]
G2A is an orphan G protein-coupled receptor (GPCR), expressed predominantly in T and B cells and homologous to a small group of GPCRs of unknown function expressed in lymphoid tissues.
Feramisco, Jamison D. +6 more
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On the hierarchical classification of G Protein-Coupled Receptors [PDF]
Motivation: G protein-coupled receptors (GPCRs) play an important role in many physiological systems by transducing an extracellular signal into an intracellular response. Over 50% of all marketed drugs are targeted towards a GPCR.
A. A. Freitas +31 more
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Roles of distinct nuclear receptors in diabetic cardiomyopathy
Diabetes mellitus induces a pathophysiological disorder known as diabetic cardiomyopathy and may eventually cause heart failure. Diabetic cardiomyopathy is manifested with systolic and diastolic contractile dysfunction along with alterations in unique ...
Yangyang Zheng +8 more
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Studying non-mammalian models? Not a fool's ERRand! [PDF]
Through studies in mammalian model systems, the estrogen-receptor-related receptor (ERR) alpha, an orphan nuclear receptor, has been shown to interfere with estrogen signaling and might therefore be an interesting pharmaceutical target in estrogen ...
Bardet, Pierre-Luc +2 more
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Nuclear receptors in metabolism and diseases: Mechanistic and therapeutic insights
Nuclear receptors (NRs) are ligand-activated transcription factors that function as metabolic sensors, integrating endogenous and xenobiotic signals to regulate gene networks controlling metabolism, immunity, and cellular homeostasis.
Chen-Ying Zhu +5 more
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Circadian regulation of reproduction: From gamete to offspring [PDF]
P01326625; Grants: GNT0519315Few challenges are more critical to the survival of a species than reproduction. To ensure reproductive success, myriad aspects of physiology and behaviour need to be tightly orchestrated within the animal, as well as timed ...
Boden, M., Kennaway, D., Varcoe, T.
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Asynchronous Rhythm of Steroidogenic Factor 1 and Period Homolog 2 mRNA Expression in Mouse Y1 Adrenocorticol Tumor Cells [PDF]
The relationship between the expression of Steroidogenic factor 1 (Sf1) and the circadian-related gene, period homolog 2 (Per2), in the adrenal cortex is still unknown.
Hajime Nawata +9 more
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