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Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Gege C, Cummings MD, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Nelen MI, Milligan C, Spurlino J, Xue X, Leonard K, Edwards JP, Fourie A, Goldberg SD, Hoffmann T. Gege C, et al. Among authors: albers m. Bioorg Med Chem Lett. 2018 May 15;28(9):1446-1455. doi: 10.1016/j.bmcl.2018.03.093. Epub 2018 Apr 3. Bioorg Med Chem Lett. 2018. PMID: 29631962
3-Substituted Quinolines as RORγt Inverse Agonists.
Tanis VM, Venkatesan H, Cummings MD, Albers M, Kent Barbay J, Herman K, Kummer DA, Milligan C, Nelen MI, Nishimura R, Schlueter T, Scott B, Spurlino J, Wolin R, Woods C, Xue X, Edwards JP, Fourie AM, Leonard K. Tanis VM, et al. Among authors: albers m. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1463-1470. doi: 10.1016/j.bmcl.2019.04.021. Epub 2019 Apr 12. Bioorg Med Chem Lett. 2019. PMID: 31010722
Discovery and optimization of new oxadiazole substituted thiazole RORγt inverse agonists through a bioisosteric amide replacement approach.
Steeneck C, Gege C, Kinzel O, Albers M, Kleymann G, Schlüter T, Schulz A, Xue X, Cummings MD, Fourie AM, Leonard KA, Scott B, Edwards JP, Hoffmann T, Goldberg SD. Steeneck C, et al. Among authors: albers m. Bioorg Med Chem Lett. 2020 Jun 15;30(12):127174. doi: 10.1016/j.bmcl.2020.127174. Epub 2020 Apr 7. Bioorg Med Chem Lett. 2020. PMID: 32334912
Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt.
Gege C, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Hoffmann T, Xue X, Cummings MD, Spurlino J, Milligan C, Fourie AM, Edwards JP, Leonard K, Coe K, Scott B, Pippel D, Goldberg SD. Gege C, et al. Among authors: albers m. Bioorg Med Chem Lett. 2020 Jun 15;30(12):127205. doi: 10.1016/j.bmcl.2020.127205. Epub 2020 Apr 21. Bioorg Med Chem Lett. 2020. PMID: 32336498
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: albers m. Sci Rep. 2016 Dec 1;6:37977. doi: 10.1038/srep37977. Sci Rep. 2016. PMID: 27905482 Free PMC article.
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: albers m. 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.
333 results