Advancements in therapeutically-targeting orphan GPCRs
Frontiers in Pharmacology, 2015 G-protein coupled receptors (GPCRs) are popular biological targets for drug discovery and development. To date there are more than 140 orphan GPCRs, i.e. receptors whose endogenous ligands are unknown.
Jennifer eStockert, Lakshmi A. Devi
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Heliyon, 2021 The identification of cannabinoid ligands Cannabidiol and O-1918 as inverse agonists of the orphan receptor GPR52 is reported. Detailed characterisation of GPR52 pharmacology and modelling of the proposed receptor interaction is described.
Lisa A. Stott +12 more
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ROR-γ drives androgen receptor expression and represents a therapeutic target in castration-resistant prostate cancer. [PDF]
, 2016 The androgen receptor (AR) is overexpressed and hyperactivated in human castration-resistant prostate cancer (CRPC). However, the determinants of AR overexpression in CRPC are poorly defined.
Borowsky, Alexander D +17 more
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A Review of Melatonin, Its Receptors and Drugs
Eurasian Journal of Medicine, 2019 After a Turkish scientist took Nobel Prize due to his contributions to understand clock genes, melatonin, closely related to these genes, may begin to shine.
Mucahit Emet +5 more
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LGR5 is associated with tumor aggressiveness in papillary thyroid cancer. [PDF]
, 2015 PurposeLeucine-rich repeat-containing G-protein-coupled receptor 5 (LGR5) is a cancer stem cell marker and a down-stream target in Wnt/β-catenin signaling. In human papillary thyroid cancer (PTC), over activation of Wnt/β-catenin has been associated with
Diehl, Anna Mae +4 more
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Prediction and classification for GPCR sequences based on ligand specific features [PDF]
, 2006 Functional identification of G-Protein Coupled Receptors (GPCRs) is one of the current focus areas of pharmaceutical research. Although thousands of GPCR sequences are known, many of them are orphan sequences (the activating ligand is unknown). Therefore,
F. Horn +8 more
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Optical functionalization of human Class A orphan G-protein-coupled receptors
Nature Communications, 2018 G-protein coupled receptors (GPCRs) represent the largest receptor family and are prime drug targets, but many orphan GPCRs are poorly characterized. Here authors engineer human orphan GPCRs to be activated by light which allows studying the receptors ...
Maurizio Morri +7 more
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Gene expression patterns following unilateral traumatic brain injury reveals a local pro-inflammatory and remote anti-inflammatory response. [PDF]
, 2013 BackgroundTraumatic brain injury (TBI) results in irreversible damage at the site of impact and initiates cellular and molecular processes that lead to secondary neural injury in the surrounding tissue.
Ford, Byron D +5 more
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Identification of COUP-TFII orphan nuclear receptor as a retinoic acid-activated receptor.
PLoS Biology, 2008 The chicken ovalbumin upstream promoter-transcription factors (COUP-TFI and II) make up the most conserved subfamily of nuclear receptors that play key roles in angiogenesis, neuronal development, organogenesis, cell fate determination, and metabolic ...
Schoen W Kruse +10 more
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Retinoid receptor-related orphan receptor alpha: a key gene setting brain circuits
Neural Regeneration Research, 2018 The retinoid receptor-related orphan receptor alpha (RORα) is thought to act as a constitutive activator of transcription by binding to the ROR response element (RORE) of target genes.
Tania Vitalis, Jean Mariani
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