134 related articles for article (PubMed ID: 26014484)
1. Design and synthesis of novel ROR inverse agonists with a dibenzosilole scaffold as a hydrophobic core structure.
Toyama H; Nakamura M; Hashimoto Y; Fujii S
Bioorg Med Chem; 2015 Jul; 23(13):2982-8. PubMed ID: 26014484
[TBL] [Abstract][Full Text] [Related]
2. Development of novel silicon-containing inverse agonists of retinoic acid receptor-related orphan receptors.
Toyama H; Nakamura M; Nakamura M; Matsumoto Y; Nakagomi M; Hashimoto Y
Bioorg Med Chem; 2014 Mar; 22(6):1948-59. PubMed ID: 24559867
[TBL] [Abstract][Full Text] [Related]
3. Discovery and structural optimization of 4-(4-(benzyloxy)phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists.
Wu XS; Wang R; Xing YL; Xue XQ; Zhang Y; Lu YZ; Song Y; Luo XY; Wu C; Zhou YL; Jiang JQ; Xu Y
Acta Pharmacol Sin; 2016 Nov; 37(11):1516-1524. PubMed ID: 27374490
[TBL] [Abstract][Full Text] [Related]
4. Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
Nishiyama Y; Nakamura M; Misawa T; Nakagomi M; Makishima M; Ishikawa M; Hashimoto Y
Bioorg Med Chem; 2014 May; 22(9):2799-808. PubMed ID: 24702856
[TBL] [Abstract][Full Text] [Related]
5. Molecular Mechanism of Action of RORγt Agonists and Inverse Agonists: Insights from Molecular Dynamics Simulation.
Sun N; Yuan C; Ma X; Wang Y; Gu X; Fu W
Molecules; 2018 Dec; 23(12):. PubMed ID: 30513894
[TBL] [Abstract][Full Text] [Related]
6. Efficient Lead Finding, Activity Enhancement and Preliminary Selectivity Control of Nuclear Receptor Ligands Bearing a Phenanthridinone Skeleton.
Nishiyama Y; Fujii S; Makishima M; Hashimoto Y; Ishikawa M
Int J Mol Sci; 2018 Jul; 19(7):. PubMed ID: 30021999
[TBL] [Abstract][Full Text] [Related]
7. Ligand-Based Design of Allosteric Retinoic Acid Receptor-Related Orphan Receptor γt (RORγt) Inverse Agonists.
Meijer FA; Doveston RG; de Vries RMJM; Vos GM; Vos AAA; Leysen S; Scheepstra M; Ottmann C; Milroy LG; Brunsveld L
J Med Chem; 2020 Jan; 63(1):241-259. PubMed ID: 31821760
[TBL] [Abstract][Full Text] [Related]
8. All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta.
Stehlin-Gaon C; Willmann D; Zeyer D; Sanglier S; Van Dorsselaer A; Renaud JP; Moras D; Schüle R
Nat Struct Biol; 2003 Oct; 10(10):820-5. PubMed ID: 12958591
[TBL] [Abstract][Full Text] [Related]
9. Identification of tertiary sulfonamides as RORc inverse agonists.
Fauber BP; René O; Burton B; Everett C; Gobbi A; Hawkins J; Johnson AR; Liimatta M; Lockey P; Norman M; Wong H
Bioorg Med Chem Lett; 2014 May; 24(9):2182-7. PubMed ID: 24685544
[TBL] [Abstract][Full Text] [Related]
10. Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.
Fauber BP; René O; Deng Y; DeVoss J; Eidenschenk C; Everett C; Ganguli A; Gobbi A; Hawkins J; Johnson AR; La H; Lesch J; Lockey P; Norman M; Ouyang W; Summerhill S; Wong H
J Med Chem; 2015 Jul; 58(13):5308-22. PubMed ID: 26061388
[TBL] [Abstract][Full Text] [Related]
11. Re-emergence of an orphan therapeutic target for the treatment of resistant prostate cancer - a thorough conformational and binding analysis for ROR-γ protein.
Ndagi U; Mhlongo NN; Soliman ME
J Biomol Struct Dyn; 2018 Feb; 36(2):335-350. PubMed ID: 28027708
[TBL] [Abstract][Full Text] [Related]
12. Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.
Kono M; Ochida A; Oda T; Imada T; Banno Y; Taya N; Masada S; Kawamoto T; Yonemori K; Nara Y; Fukase Y; Yukawa T; Tokuhara H; Skene R; Sang BC; Hoffman ID; Snell GP; Uga K; Shibata A; Igaki K; Nakamura Y; Nakagawa H; Tsuchimori N; Yamasaki M; Shirai J; Yamamoto S
J Med Chem; 2018 Apr; 61(7):2973-2988. PubMed ID: 29510038
[TBL] [Abstract][Full Text] [Related]
13. Probing the Hydrophobic Binding Pocket of G-Protein-Coupled Lysophosphatidylserine Receptor GPR34/LPS
Sayama M; Inoue A; Nakamura S; Jung S; Ikubo M; Otani Y; Uwamizu A; Kishi T; Makide K; Aoki J; Hirokawa T; Ohwada T
J Med Chem; 2017 Jul; 60(14):6384-6399. PubMed ID: 28715213
[TBL] [Abstract][Full Text] [Related]
14. Discovery of phenoxyindazoles and phenylthioindazoles as RORγ inverse agonists.
Ouvry G; Bouix-Peter C; Ciesielski F; Chantalat L; Christin O; Comino C; Duvert D; Feret C; Harris CS; Lamy L; Luzy AP; Musicki B; Orfila D; Pascau J; Parnet V; Perrin A; Pierre R; Polge G; Raffin C; Rival Y; Taquet N; Thoreau E; Hennequin LF
Bioorg Med Chem Lett; 2016 Dec; 26(23):5802-5808. PubMed ID: 27815118
[TBL] [Abstract][Full Text] [Related]
15. Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.
Fauber BP; René O; de Leon Boenig G; Burton B; Deng Y; Eidenschenk C; Everett C; Gobbi A; Hymowitz SG; Johnson AR; La H; Liimatta M; Lockey P; Norman M; Ouyang W; Wang W; Wong H
Bioorg Med Chem Lett; 2014 Aug; 24(16):3891-7. PubMed ID: 25017032
[TBL] [Abstract][Full Text] [Related]
16. Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist.
Yukawa T; Nara Y; Kono M; Sato A; Oda T; Takagi T; Sato T; Banno Y; Taya N; Imada T; Shiokawa Z; Negoro N; Kawamoto T; Koyama R; Uchiyama N; Skene R; Hoffman I; Chen CH; Sang B; Snell G; Katsuyama R; Yamamoto S; Shirai J
J Med Chem; 2019 Feb; 62(3):1167-1179. PubMed ID: 30652849
[TBL] [Abstract][Full Text] [Related]
17. Structure-Based Design and Synthesis of Fluorene Derivatives as Novel RORγt Inverse Agonists.
Gabr MT; Abdel-Raziq MS
Chem Biodivers; 2018 Sep; 15(9):e1800244. PubMed ID: 29935095
[TBL] [Abstract][Full Text] [Related]
18. A Drug with Lipophilicity-Dependent Potency Can Be Metabolically Stable: Discovery of a Potent and Selective Retinoic Acid Receptor-Related Orphan Receptor C2 (RORC2) Inverse Agonist as an Orally Bioavailable Anti-Inflammatory Agent.
Wang Y; Liu H
J Med Chem; 2018 Dec; 61(23):10412-10414. PubMed ID: 30507131
[TBL] [Abstract][Full Text] [Related]
19. Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
Gege C; Schlüter T; Hoffmann T
Bioorg Med Chem Lett; 2014 Nov; 24(22):5265-7. PubMed ID: 25305688
[TBL] [Abstract][Full Text] [Related]
20. Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.
Fauber BP; Gobbi A; Savy P; Burton B; Deng Y; Everett C; La H; Johnson AR; Lockey P; Norman M; Wong H
Bioorg Med Chem Lett; 2015 Oct; 25(19):4109-13. PubMed ID: 26321361
[TBL] [Abstract][Full Text] [Related]
[Next] [New Search]
