PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 32683181-4 2020 We successfully engineered high affinity ERRalpha agonism into a chemical scaffold that displays selective ERRbeta/gamma agonist activity (GSK4716), providing novel ERRalpha/beta/gamma pan agonists that can be used as tools to probe the physiological roles of these nuclear receptors. GSK 4716 139-146 estrogen related receptor alpha Homo sapiens 41-49 33612148-5 2021 Interestingly, GSK5182 increased ERRgamma protein levels much as does GSK4716, which is an ERRgamma agonist. GSK 4716 70-77 estrogen related receptor gamma Homo sapiens 91-99 32897058-5 2020 Here, we describe a novel dual ERRalpha/gamma inverse agonist, SLU-PP-1072, derived from the GSK4716 ERRgamma agonist scaffold that is distinct from the XCT790 scaffold. GSK 4716 93-100 estrogen related receptor alpha Homo sapiens 31-39 32897058-5 2020 Here, we describe a novel dual ERRalpha/gamma inverse agonist, SLU-PP-1072, derived from the GSK4716 ERRgamma agonist scaffold that is distinct from the XCT790 scaffold. GSK 4716 93-100 estrogen related receptor gamma Homo sapiens 101-109 32683181-4 2020 We successfully engineered high affinity ERRalpha agonism into a chemical scaffold that displays selective ERRbeta/gamma agonist activity (GSK4716), providing novel ERRalpha/beta/gamma pan agonists that can be used as tools to probe the physiological roles of these nuclear receptors. GSK 4716 139-146 estrogen related receptor alpha Homo sapiens 107-120 32683181-4 2020 We successfully engineered high affinity ERRalpha agonism into a chemical scaffold that displays selective ERRbeta/gamma agonist activity (GSK4716), providing novel ERRalpha/beta/gamma pan agonists that can be used as tools to probe the physiological roles of these nuclear receptors. GSK 4716 139-146 estrogen related receptor alpha Homo sapiens 165-178 32173553-5 2020 The ERRgamma agonist GSK4716 increased DAT and TH expression, and the ERRgamma inverse agonist GSK5182 attenuated the retinoic acid-induced upregulation of DAT and TH in differentiated SH-SY5Y cells. GSK 4716 21-28 tyrosine hydroxylase Homo sapiens 47-49 32173553-0 2020 Regulation of dopaminergic neuronal phenotypes by the estrogen-related receptor gamma ligand GSK4716 via the activation of CREB signaling. GSK 4716 93-100 estrogen related receptor gamma Homo sapiens 54-85 32173553-5 2020 The ERRgamma agonist GSK4716 increased DAT and TH expression, and the ERRgamma inverse agonist GSK5182 attenuated the retinoic acid-induced upregulation of DAT and TH in differentiated SH-SY5Y cells. GSK 4716 21-28 solute carrier family 6 member 3 Homo sapiens 156-159 32173553-0 2020 Regulation of dopaminergic neuronal phenotypes by the estrogen-related receptor gamma ligand GSK4716 via the activation of CREB signaling. GSK 4716 93-100 cAMP responsive element binding protein 1 Homo sapiens 123-127 32173553-5 2020 The ERRgamma agonist GSK4716 increased DAT and TH expression, and the ERRgamma inverse agonist GSK5182 attenuated the retinoic acid-induced upregulation of DAT and TH in differentiated SH-SY5Y cells. GSK 4716 21-28 tyrosine hydroxylase Homo sapiens 164-166 32173553-5 2020 The ERRgamma agonist GSK4716 increased DAT and TH expression, and the ERRgamma inverse agonist GSK5182 attenuated the retinoic acid-induced upregulation of DAT and TH in differentiated SH-SY5Y cells. GSK 4716 21-28 solute carrier family 6 member 3 Homo sapiens 39-42 32173553-6 2020 We found that biphasic activation of the protein kinase A/cyclic AMP response element-binding (CREB) protein signaling pathway was involved in the GSK4716-induced increase in the DAergic phenotype in SH-SY5Y cells. GSK 4716 147-154 cAMP responsive element binding protein 1 Homo sapiens 95-99 32173553-7 2020 CREB signaling activated as early as 3 h after GSK4716 treatment in an ERRgamma-independent manner, but increased following ERRgamma activation after 3 days. GSK 4716 47-54 cAMP responsive element binding protein 1 Homo sapiens 0-4 32173553-8 2020 Protein kinase A inhibitor H-89 attenuated GSK4716-induced DAT and TH upregulation. GSK 4716 43-50 solute carrier family 6 member 3 Homo sapiens 59-62 32173553-9 2020 In primary cultured DAergic neurons, GSK4716 increased neurite length and the number of DAT and TH-double-positive (DAT+TH+) neurons compared to that in control cells. GSK 4716 37-44 solute carrier family 6 member 3 Homo sapiens 88-91 32173553-9 2020 In primary cultured DAergic neurons, GSK4716 increased neurite length and the number of DAT and TH-double-positive (DAT+TH+) neurons compared to that in control cells. GSK 4716 37-44 solute carrier family 6 member 3 Homo sapiens 116-119 31491697-5 2019 All of the tested chemicals could bind to ERRgamma with the Kd (dissociation constant) values ranging from not available (NA) to 3.2 muM 4"-OH-PCB 12 showed the highest binding affinity with Kd value of 3.2 muM, which was comparable to that of a synthetic ERRgamma agonist GSK4716. GSK 4716 273-280 estrogen related receptor gamma Homo sapiens 42-50 22457827-7 2012 Conversely, stimulation of ERRbeta with a selective agonist (GSK4716) in a TAL cell line stimulated NKCC2 expression. GSK 4716 61-68 estrogen related receptor, beta Mus musculus 27-34 22457827-7 2012 Conversely, stimulation of ERRbeta with a selective agonist (GSK4716) in a TAL cell line stimulated NKCC2 expression. GSK 4716 61-68 solute carrier family 12, member 1 Mus musculus 100-105 19631715-2 2010 Natural ligands have not been identified, however, recent reports have demonstrated the synthetic phenolic acyl hydrazone, GSK4716, functions as a selective ERRbeta/gamma agonist. GSK 4716 123-130 estrogen related receptor beta Homo sapiens 157-170 19631715-4 2010 Treatment of differentiated skeletal muscle cells with the ERRbeta/gamma agonist (GSK4716) produced a significant increase in the expression of GRalpha (isoform D) protein. GSK 4716 82-89 estrogen related receptor beta Homo sapiens 59-72 16990259-7 2006 The observed agonist-bound state contains the ERRgamma LBD, a ligand (GSK4716), and the RIP140 peptide and reveals an unexpected rearrangement of the phenol-binding residues. GSK 4716 70-77 estrogen related receptor gamma Homo sapiens 46-54 18776219-9 2008 In addition, the ERRgamma agonist GSK4716 induced miR-433 and miR-127 expression both in vitro and in vivo, respectively. GSK 4716 34-41 microRNA 433 Mus musculus 50-57 18776219-9 2008 In addition, the ERRgamma agonist GSK4716 induced miR-433 and miR-127 expression both in vitro and in vivo, respectively. GSK 4716 34-41 microRNA 127 Mus musculus 62-69 16990259-7 2006 The observed agonist-bound state contains the ERRgamma LBD, a ligand (GSK4716), and the RIP140 peptide and reveals an unexpected rearrangement of the phenol-binding residues. GSK 4716 70-77 nuclear receptor interacting protein 1 Homo sapiens 88-94 16990259-9 2006 In contrast to the conventional mechanism of nuclear receptor ligand activation, activation of ERRgamma by GSK4716 does not appear to involve a major rearrangement or significant stabilization of the C-terminal helix. GSK 4716 107-114 estrogen related receptor gamma Homo sapiens 95-103 15857113-2 2005 GSK4716 (3) and GSK9089 (4) show binding to ERRgamma with remarkable selectivity over the classical estrogen receptors. GSK 4716 0-7 estrogen related receptor gamma Homo sapiens 44-52 16515477-7 2006 The phenolic acyl hydrazones GSK4716 and GSK9089 act as selective agonists of ERRbeta and ERRgamma. GSK 4716 29-36 estrogen related receptor beta Homo sapiens 78-85 16515477-7 2006 The phenolic acyl hydrazones GSK4716 and GSK9089 act as selective agonists of ERRbeta and ERRgamma. GSK 4716 29-36 estrogen related receptor gamma Homo sapiens 90-98