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Human T-bet+ B cell development is associated with BTK activity and suppressed by evobrutinib.
Rijvers L, van Langelaar J, Bogers L, Melief MJ, Koetzier SC, Blok KM, Wierenga-Wolf AF, de Vries HE, Rip J, Corneth OB, Hendriks RW, Grenningloh R, Boschert U, Smolders J, van Luijn MM. Rijvers L, et al. Among authors: grenningloh r. JCI Insight. 2022 Aug 22;7(16):e160909. doi: 10.1172/jci.insight.160909. JCI Insight. 2022. PMID: 35852869 Free PMC article.
Bruton's Tyrosine Kinase Inhibition Promotes Myelin Repair.
Martin E, Aigrot MS, Grenningloh R, Stankoff B, Lubetzki C, Boschert U, Zalc B. Martin E, et al. Among authors: grenningloh r. Brain Plast. 2020 Oct 1;5(2):123-133. doi: 10.3233/BPL-200100. Brain Plast. 2020. PMID: 33282676 Free PMC article.
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L. Caldwell RD, et al. Among authors: grenningloh r. J Med Chem. 2019 Sep 12;62(17):7643-7655. doi: 10.1021/acs.jmedchem.9b00794. Epub 2019 Aug 15. J Med Chem. 2019. PMID: 31368705
Btk inhibition treats TLR7/IFN driven murine lupus.
Bender AT, Pereira A, Fu K, Samy E, Wu Y, Liu-Bujalski L, Caldwell R, Chen YY, Tian H, Morandi F, Head J, Koehler U, Genest M, Okitsu SL, Xu D, Grenningloh R. Bender AT, et al. Among authors: grenningloh r. Clin Immunol. 2016 Mar;164:65-77. doi: 10.1016/j.clim.2016.01.012. Epub 2016 Jan 25. Clin Immunol. 2016. PMID: 26821304 Free article.
Discovery of potent, highly selective covalent irreversible BTK inhibitors from a fragment hit.
Qiu H, Liu-Bujalski L, Caldwell RD, Follis AV, Gardberg A, Goutopoulos A, Grenningloh R, Head J, Johnson T, Jones R, Mochalkin I, Morandi F, Neagu C, Sherer B. Qiu H, et al. Among authors: grenningloh r. Bioorg Med Chem Lett. 2018 Sep 15;28(17):2939-2944. doi: 10.1016/j.bmcl.2018.07.008. Epub 2018 Jul 5. Bioorg Med Chem Lett. 2018. PMID: 30122225
Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk.
Caldwell R, Liu-Bujalski L, Qiu H, Mochalkin I, Jones R, Neagu C, Goutopoulos A, Grenningloh R, Johnson T, Sherer B, Gardberg A, Follis AV, Morandi F, Head J. Caldwell R, et al. Among authors: grenningloh r. Bioorg Med Chem Lett. 2018 Nov 15;28(21):3419-3424. doi: 10.1016/j.bmcl.2018.09.033. Epub 2018 Sep 27. Bioorg Med Chem Lett. 2018. PMID: 30290988
32 results