Investigation of selective retinoic acid receptor alpha antagonist ER-50891 and related analogs for male contraception.
Sign Up to like & getrecommendations! Published in 2023 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202300031
Abstract: Retinoic acid receptor alpha (RARα) antagonist ER-50891 and 15 analogs were prepared and tested in vitro for potency and selectivity at RARα, RARβ, and RARγ using transactivation assays. Minor modifications to the parent molecule such… read more here.
Keywords: receptor alpha; antagonist 50891; retinoic acid; acid receptor ... See more keywords
Retinoic acid receptor gamma is required for proliferation of pancreatic cancer cells
Sign Up to like & getrecommendations! Published in 2022 at "Cell Biology International"
DOI: 10.1002/cbin.11917
Abstract: Despite the expectation that retinoic acid receptor could be the potential therapeutic targets for pancreatic cancers, there has been the lack of information about the role and the impact of retinoic acid receptor gamma (RARγ,… read more here.
Keywords: proliferation; pancreatic cancer; retinoic acid; acid receptor ... See more keywords
Analysis of Retinoic Acid Receptor Signaling in Colorectal Cancer.
Sign Up to like & getrecommendations! Published in 2019 at "Methods in molecular biology"
DOI: 10.1007/978-1-4939-9585-1_6
Abstract: Retinoic acid receptor (RAR) signaling plays an important role in embryonic development and homeostasis of many tissues. At the cellular level, activation of RAR signaling often induces cell cycle arrest, differentiation, and apoptosis in many… read more here.
Keywords: acid receptor; colorectal cancer; retinoic acid; signaling colorectal ... See more keywords
The retinoic acid receptor (RAR) in molluscs: Function, evolution and endocrine disruption insights.
Sign Up to like & getrecommendations! Published in 2019 at "Aquatic toxicology"
DOI: 10.1016/j.aquatox.2019.01.002
Abstract: Retinoid acid receptor (RAR)-dependent signalling pathways are essential for the regulation and maintenance of essential biological functions and are recognized targets of disruptive anthropogenic compounds. Recent studies put forward the inability of mollusc RARs to… read more here.
Keywords: rar; acid receptor; function; receptor rar ... See more keywords
IL‐33 stimulates expression of the GPR84 (EX33) fatty acid receptor gene and of cytokine and chemokine genes in human adipocytes
Sign Up to like & getrecommendations! Published in 2018 at "Cytokine"
DOI: 10.1016/j.cyto.2018.05.008
Abstract: HighlightsIL‐33 stimulates expression of the GPR84 fatty acid receptor gene in human adipocytes.IL‐33 also induces strong expression of the IL1B, CCL2, IL6, CXCL2 and CSF3 genes.ADIPOQ (adiponectin) expression is not altered by IL‐33.Secretion of G‐CSF… read more here.
Keywords: acid receptor; fatty acid; expression; expression gpr84 ... See more keywords
Modulation of immune responses by bile acid receptor agonists in myasthenia gravis
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Neuroimmunology"
DOI: 10.1016/j.jneuroim.2020.577397
Abstract: Bile acids bind to multiple receptors, including Takeda G protein-coupled receptor 5 (TGR5) and farnesoid-X-receptors alpha (FXRα). We compared the response of PBMCs to the activation of these receptors in healthy controls and myasthenic patients.… read more here.
Keywords: acid receptor; immune responses; modulation immune; responses bile ... See more keywords
Interplay of Protein Disorder in Retinoic Acid Receptor Heterodimer and Its Corepressor Regulates Gene Expression.
Sign Up to like & getrecommendations! Published in 2019 at "Structure"
DOI: 10.1016/j.str.2019.05.001
Abstract: In its unliganded form, the retinoic acid receptor (RAR) in heterodimer with the retinoid X receptor (RXR) exerts a strong repressive activity facilitated by the recruitment of transcriptional corepressors in the promoter region of target… read more here.
Keywords: receptor; rar; acid receptor; retinoic acid ... See more keywords
Activating Effects of Phenolics from Apache Red Zea mays L. on Free Fatty Acid Receptor 1 and Glucokinase Evaluated with a Dual Culture System with Epithelial, Pancreatic, and Liver Cells.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of agricultural and food chemistry"
DOI: 10.1021/acs.jafc.8b06642
Abstract: The aim was to characterize a phenolic-rich water extract from the pericarp of an improved genotype of Apache red maize (RPE) and evaluate its ability to activate the type 2 diabetes markers free fatty acid… read more here.
Keywords: acid receptor; apache red; fatty acid; free fatty ... See more keywords
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b00392
Abstract: The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of the receptor is anticipated to… read more here.
Keywords: acid receptor; inverse agonist; receptor related; retinoic acid ... See more keywords
Structure–Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.9b02036
Abstract: Free fatty acid receptor 3 (FFA3, previously GPR41) is activated by short-chain fatty acids, mediates health effects of the gut microbiota, and is a therapeutic target for metabolic and inflammatory diseases. The shortage of well-characterized… read more here.
Keywords: fatty acid; free fatty; activity relationship; structure activity ... See more keywords
A potent free fatty acid receptor 1 agonist with a glucose-dependent antihyperglycemic effect.
Sign Up to like & getrecommendations! Published in 2019 at "Chemical communications"
DOI: 10.1039/c9cc04040d
Abstract: We present a novel free fatty acid receptor 1 (FFA1) agonist, named PAFA, with a strong agonist potency (EC50 = 6.04 nM) and good serum stability. PAFA significantly stimulates insulin secretion in INS-1 cells in… read more here.
Keywords: agonist; fatty acid; free fatty; acid receptor ... See more keywords