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Ability of Bruton's Tyrosine Kinase Inhibitors to Sequester Y551 and Prevent Phosphorylation Determines Potency for Inhibition of Fc Receptor but not B-Cell Receptor Signaling.
Bender AT, Gardberg A, Pereira A, Johnson T, Wu Y, Grenningloh R, Head J, Morandi F, Haselmayer P, Liu-Bujalski L. Bender AT, et al. Among authors: grenningloh r. Mol Pharmacol. 2017 Mar;91(3):208-219. doi: 10.1124/mol.116.107037. Epub 2017 Jan 6. Mol Pharmacol. 2017. PMID: 28062735
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.
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.
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
Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors.
Qiu H, Ali Z, Bender A, Caldwell R, Chen YY, Fang Z, Gardberg A, Glaser N, Goettsche A, Goutopoulos A, Grenningloh R, Hanschke B, Head J, Johnson T, Jones C, Jones R, Kulkarni S, Maurer C, Morandi F, Neagu C, Poetzsch S, Potnick J, Schmidt R, Roe K, Viacava Follis A, Wing C, Zhu X, Sherer B. Qiu H, et al. Among authors: grenningloh r. Bioorg Med Chem. 2021 Jun 15;40:116163. doi: 10.1016/j.bmc.2021.116163. Epub 2021 Apr 20. Bioorg Med Chem. 2021. PMID: 33932711
Characterization of Novel PI3Kδ Inhibitors as Potential Therapeutics for SLE and Lupus Nephritis in Pre-Clinical Studies.
Haselmayer P, Camps M, Muzerelle M, El Bawab S, Waltzinger C, Bruns L, Abla N, Polokoff MA, Jond-Necand C, Gaudet M, Benoit A, Bertschy Meier D, Martin C, Gretener D, Lombardi MS, Grenningloh R, Ladel C, Petersen JS, Gaillard P, Ji H. Haselmayer P, et al. Among authors: grenningloh r. Front Immunol. 2014 May 22;5:233. doi: 10.3389/fimmu.2014.00233. eCollection 2014. Front Immunol. 2014. PMID: 24904582 Free PMC article.
Discovery of Covalent Bruton's Tyrosine Kinase Inhibitors with Decreased CYP2C8 Inhibitory Activity.
Qiu H, Ali Z, Bowlan J, Caldwell R, Gardberg A, Glaser N, Goutopoulos A, Head J, Johnson T, Maurer C, Georgi K, Grenningloh R, Fang Z, Morandi F, Rohdich F, Schmidt R, Follis AV, Sherer B. Qiu H, et al. Among authors: grenningloh r. ChemMedChem. 2021 Dec 14;16(24):3653-3662. doi: 10.1002/cmdc.202100453. Epub 2021 Oct 8. ChemMedChem. 2021. PMID: 34582626
32 results