BIOMARKERS

Molecular Biopsy of Human Tumors

- a resource for Precision Medicine *

177 related articles for article (PubMed ID: 29327456)

  • 1. Discovery and Characterization of CD12681, a Potent RORγ Inverse Agonist, Preclinical Candidate for the Topical Treatment of Psoriasis.
    Ouvry G; Atrux-Tallau N; Bihl F; Bondu A; Bouix-Peter C; Carlavan I; Christin O; Cuadrado MJ; Defoin-Platel C; Deret S; Duvert D; Feret C; Forissier M; Fournier JF; Froude D; Hacini-Rachinel F; Harris CS; Hervouet C; Huguet H; Lafitte G; Luzy AP; Musicki B; Orfila D; Ozello B; Pascau C; Pascau J; Parnet V; Peluchon G; Pierre R; Piwnica D; Raffin C; Rossio P; Spiesse D; Taquet N; Thoreau E; Vatinel R; Vial E; Hennequin LF
    ChemMedChem; 2018 Feb; 13(4):321-337. PubMed ID: 29327456
    [TBL] [Abstract][Full Text] [Related]  

  • 2. 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]  

  • 3. Discovery of novel N-sulfonamide-tetrahydroquinolines as potent retinoic acid receptor-related orphan receptor γt inverse agonists for the treatment of autoimmune diseases.
    Sun N; Ma X; Zhou K; Zhu C; Cao Z; Wang Y; Xu J; Fu W
    Eur J Med Chem; 2020 Feb; 187():111984. PubMed ID: 31881455
    [TBL] [Abstract][Full Text] [Related]  

  • 4. Discovery of a novel RORγ antagonist with skin-restricted exposure for topical treatment of mild to moderate psoriasis.
    Liu S; Liu D; Shen R; Li D; Hu Q; Yan Y; Sun J; Zhang F; Wan H; Dong P; Feng J; Zhang R; Li J; Zhang L; Tao W
    Sci Rep; 2021 Apr; 11(1):9132. PubMed ID: 33911101
    [TBL] [Abstract][Full Text] [Related]  

  • 5. Discovery and Optimization of a Series of Sulfonamide Inverse Agonists for the Retinoic Acid Receptor-Related Orphan Receptor-α.
    Doebelin C; He Y; Campbell S; Nuhant P; Kumar N; Koenig M; Garcia-Ordonez R; Chang MR; Roush WR; Lin L; Kahn S; Cameron MD; Griffin PR; Solt LA; Kamenecka TM
    Med Chem; 2019; 15(6):676-684. PubMed ID: 30799793
    [TBL] [Abstract][Full Text] [Related]  

  • 6. Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin.
    Smith SH; Peredo CE; Takeda Y; Bui T; Neil J; Rickard D; Millerman E; Therrien JP; Nicodeme E; Brusq JM; Birault V; Viviani F; Hofland H; Jetten AM; Cote-Sierra J
    PLoS One; 2016; 11(2):e0147979. PubMed ID: 26870941
    [TBL] [Abstract][Full Text] [Related]  

  • 7. 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.
    Schnute ME; Wennerstål M; Alley J; Bengtsson M; Blinn JR; Bolten CW; Braden T; Bonn T; Carlsson B; Caspers N; Chen M; Choi C; Collis LP; Crouse K; Färnegårdh M; Fennell KF; Fish S; Flick AC; Goos-Nilsson A; Gullberg H; Harris PK; Heasley SE; Hegen M; Hromockyj AE; Hu X; Husman B; Janosik T; Jones P; Kaila N; Kallin E; Kauppi B; Kiefer JR; Knafels J; Koehler K; Kruger L; Kurumbail RG; Kyne RE; Li W; Löfstedt J; Long SA; Menard CA; Mente S; Messing D; Meyers MJ; Napierata L; Nöteberg D; Nuhant P; Pelc MJ; Prinsen MJ; Rhönnstad P; Backström-Rydin E; Sandberg J; Sandström M; Shah F; Sjöberg M; Sundell A; Taylor AP; Thorarensen A; Trujillo JI; Trzupek JD; Unwalla R; Vajdos FF; Weinberg RA; Wood DC; Xing L; Zamaratski E; Zapf CW; Zhao Y; Wilhelmsson A; Berstein G
    J Med Chem; 2018 Dec; 61(23):10415-10439. PubMed ID: 30130103
    [TBL] [Abstract][Full Text] [Related]  

  • 8. Benzoxazepines Achieve Potent Suppression of IL-17 Release in Human T-Helper 17 (TH 17) Cells through an Induced-Fit Binding Mode to the Nuclear Receptor RORγ.
    Olsson RI; Xue Y; von Berg S; Aagaard A; McPheat J; Hansson EL; Bernström J; Hansson P; Jirholt J; Grindebacke H; Leffler A; Chen R; Xiong Y; Ge H; Hansson TG; Narjes F
    ChemMedChem; 2016 Jan; 11(2):207-16. PubMed ID: 26553345
    [TBL] [Abstract][Full Text] [Related]  

  • 9. 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]  

  • 10. Identification of N-phenyl-2-(N-phenylphenylsulfonamido)acetamides as new RORγ inverse agonists: Virtual screening, structure-based optimization, and biological evaluation.
    Song Y; Xue X; Wu X; Wang R; Xing Y; Yan W; Zhou Y; Qian CN; Zhang Y; Xu Y
    Eur J Med Chem; 2016 Jun; 116():13-26. PubMed ID: 27043267
    [TBL] [Abstract][Full Text] [Related]  

  • 11. Identification of novel quinazolinedione derivatives as RORγt inverse agonist.
    Fukase Y; Sato A; Tomata Y; Ochida A; Kono M; Yonemori K; Koga K; Okui T; Yamasaki M; Fujitani Y; Nakagawa H; Koyama R; Nakayama M; Skene R; Sang BC; Hoffman I; Shirai J; Yamamoto S
    Bioorg Med Chem; 2018 Feb; 26(3):721-736. PubMed ID: 29342416
    [TBL] [Abstract][Full Text] [Related]  

  • 12. Pharmacologic modulation of RORγt translates to efficacy in preclinical and translational models of psoriasis and inflammatory arthritis.
    Xue X; Soroosh P; De Leon-Tabaldo A; Luna-Roman R; Sablad M; Rozenkrants N; Yu J; Castro G; Banie H; Fung-Leung WP; Santamaria-Babi L; Schlueter T; Albers M; Leonard K; Budelsky AL; Fourie AM
    Sci Rep; 2016 Dec; 6():37977. PubMed ID: 27905482
    [TBL] [Abstract][Full Text] [Related]  

  • 13. Sulfoximines as potent RORγ inverse agonists.
    Ouvry G; Bihl F; Bouix-Peter C; Christin O; Defoin-Platel C; Deret S; Feret C; Froude D; Hacini-Rachinel F; Harris CS; Hervouet C; Lafitte G; Luzy AP; Musicki B; Orfila D; Parnet V; Pascau C; Pascau J; Pierre R; Raffin C; Rossio P; Spiesse D; Taquet N; Thoreau E; Vatinel R; Vial E; Hennequin LF
    Bioorg Med Chem Lett; 2018 May; 28(8):1269-1273. PubMed ID: 29571573
    [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. Discovery of novel pyrazole-containing benzamides as potent RORγ inverse agonists.
    Wang T; Banerjee D; Bohnert T; Chao J; Enyedy I; Fontenot J; Guertin K; Jones H; Lin EY; Marcotte D; Talreja T; Van Vloten K
    Bioorg Med Chem Lett; 2015 Aug; 25(15):2985-90. PubMed ID: 26048789
    [TBL] [Abstract][Full Text] [Related]  

  • 16. Recent progress on nuclear receptor RORγ modulators.
    Cyr P; Bronner SM; Crawford JJ
    Bioorg Med Chem Lett; 2016 Sep; 26(18):4387-4393. PubMed ID: 27542308
    [TBL] [Abstract][Full Text] [Related]  

  • 17. Small molecule mediated inhibition of RORγ-dependent gene expression and autoimmune disease pathology in vivo.
    Banerjee D; Zhao L; Wu L; Palanichamy A; Ergun A; Peng L; Quigley C; Hamann S; Dunstan R; Cullen P; Allaire N; Guertin K; Wang T; Chao J; Loh C; Fontenot JD
    Immunology; 2016 Apr; 147(4):399-413. PubMed ID: 26694902
    [TBL] [Abstract][Full Text] [Related]  

  • 18. Pharmacological inhibitory profile of TAK-828F, a potent and selective orally available RORγt inverse agonist.
    Shibata A; Uga K; Sato T; Sagara M; Igaki K; Nakamura Y; Ochida A; Kono M; Shirai J; Yamamoto S; Yamasaki M; Tsuchimori N
    Biochem Pharmacol; 2018 Apr; 150():35-45. PubMed ID: 29369782
    [TBL] [Abstract][Full Text] [Related]  

  • 19. Inhibition of Interleukin-23-Mediated Inflammation with a Novel Small Molecule Inverse Agonist of ROR
    Gauld SB; Jacquet S; Gauvin D; Wallace C; Wang Y; McCarthy R; Goess C; Leys L; Huang S; Su Z; Edelmayer R; Wetter J; Salte K; McGaraughty SP; Argiriadi MA; Honore P; Luccarini JM; Bressac D; Desino K; Breinlinger E; Cusack K; Potin D; Kort ME; Masson PJ
    J Pharmacol Exp Ther; 2019 Oct; 371(1):208-218. PubMed ID: 31375639
    [TBL] [Abstract][Full Text] [Related]  

  • 20. Discovery of a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor, S18-000003.
    Sasaki Y; Odan M; Yamamoto S; Kida S; Ueyama A; Shimizu M; Haruna T; Watanabe A; Okuno T
    Bioorg Med Chem Lett; 2018 Dec; 28(22):3549-3553. PubMed ID: 30301676
    [TBL] [Abstract][Full Text] [Related]  

    [Next]    [New Search]
    of 9.