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Preclinical and clinical characterization of the RORγt inhibitor JNJ-61803534.
Xue X, De Leon-Tabaldo A, Luna-Roman R, Castro G, Albers M, Schoetens F, DePrimo S, Devineni D, Wilde T, Goldberg S, Kinzel O, Hoffmann T, Fourie AM, Thurmond RL. Xue X, et al. Among authors: castro g. Sci Rep. 2021 May 26;11(1):11066. doi: 10.1038/s41598-021-90497-9. Sci Rep. 2021. PMID: 34040108 Free PMC article. Clinical Trial.
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. Xue X, et al. Among authors: castro g. Sci Rep. 2016 Dec 1;6:37977. doi: 10.1038/srep37977. Sci Rep. 2016. PMID: 27905482 Free PMC article.
RORγt and RORα signature genes in human Th17 cells.
Castro G, Liu X, Ngo K, De Leon-Tabaldo A, Zhao S, Luna-Roman R, Yu J, Cao T, Kuhn R, Wilkinson P, Herman K, Nelen MI, Blevitt J, Xue X, Fourie A, Fung-Leung WP. Castro G, et al. PLoS One. 2017 Aug 1;12(8):e0181868. doi: 10.1371/journal.pone.0181868. eCollection 2017. PLoS One. 2017. PMID: 28763457 Free PMC article.
Oxysterols are agonist ligands of RORγt and drive Th17 cell differentiation.
Soroosh P, Wu J, Xue X, Song J, Sutton SW, Sablad M, Yu J, Nelen MI, Liu X, Castro G, Luna R, Crawford S, Banie H, Dandridge RA, Deng X, Bittner A, Kuei C, Tootoonchi M, Rozenkrants N, Herman K, Gao J, Yang XV, Sachen K, Ngo K, Fung-Leung WP, Nguyen S, de Leon-Tabaldo A, Blevitt J, Zhang Y, Cummings MD, Rao T, Mani NS, Liu C, McKinnon M, Milla ME, Fourie AM, Sun S. Soroosh P, et al. Among authors: castro g. Proc Natl Acad Sci U S A. 2014 Aug 19;111(33):12163-8. doi: 10.1073/pnas.1322807111. Epub 2014 Aug 4. Proc Natl Acad Sci U S A. 2014. PMID: 25092323 Free PMC article.
Identification and structure activity relationships of quinoline tertiary alcohol modulators of RORγt.
Kummer DA, Cummings MD, Abad M, Barbay J, Castro G, Wolin R, Kreutter KD, Maharoof U, Milligan C, Nishimura R, Pierce J, Schalk-Hihi C, Spurlino J, Urbanski M, Venkatesan H, Wang A, Woods C, Xue X, Edwards JP, Fourie AM, Leonard K. Kummer DA, et al. Among authors: castro g. Bioorg Med Chem Lett. 2017 May 1;27(9):2047-2057. doi: 10.1016/j.bmcl.2017.02.044. Epub 2017 Feb 21. Bioorg Med Chem Lett. 2017. PMID: 28318945
6-Substituted quinolines as RORγt inverse agonists.
Barbay JK, Cummings MD, Abad M, Castro G, Kreutter KD, Kummer DA, Maharoof U, Milligan C, Nishimura R, Pierce J, Schalk-Hihi C, Spurlino J, Tanis VM, Urbanski M, Venkatesan H, Wang A, Woods C, Wolin R, Xue X, Edwards JP, Fourie AM, Leonard K. Barbay JK, et al. Among authors: castro g. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5277-5283. doi: 10.1016/j.bmcl.2017.10.027. Epub 2017 Oct 16. Bioorg Med Chem Lett. 2017. PMID: 29079472
Immunological characterization of HM5023507, an orally active PI3Kδ/γ inhibitor.
Cai Y, Yu J, Ren P, He J, Wu Z, Xiao K, Jia H, Wang J, Sai Y, Dai G, Li X, Su W, Ngo K, Castro G, Acton PD, Fung-Leung WP, Edwards JP, Venable J, Rao TS. Cai Y, et al. Among authors: castro g. Pharmacol Res Perspect. 2020 Jan 13;8(1):e00559. doi: 10.1002/prp2.559. eCollection 2020 Feb. Pharmacol Res Perspect. 2020. PMID: 31956418 Free PMC article.
1,410 results