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Items: 25

1.

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.

J Med Chem. 2019 Sep 12;62(17):7643-7655. doi: 10.1021/acs.jmedchem.9b00794. Epub 2019 Aug 15.

PMID:
31368705
2.

Efficacy and Pharmacodynamic Modeling of the BTK Inhibitor Evobrutinib in Autoimmune Disease Models.

Haselmayer P, Camps M, Liu-Bujalski L, Nguyen N, Morandi F, Head J, O'Mahony A, Zimmerli SC, Bruns L, Bender AT, Schroeder P, Grenningloh R.

J Immunol. 2019 May 15;202(10):2888-2906. doi: 10.4049/jimmunol.1800583. Epub 2019 Apr 15.

3.

A randomized, double-blind, placebo-controlled phase 1 study of multiple ascending doses of subcutaneous M1095, an anti-interleukin 17A/F nanobody, in moderate-to-severe psoriasis.

Svecova D, Lubell MW, Casset-Semanaz F, Mackenzie H, Grenningloh R, Krueger JG.

J Am Acad Dermatol. 2019 Jul;81(1):196-203. doi: 10.1016/j.jaad.2019.03.056. Epub 2019 Mar 27.

4.

Discovery of Affinity-Based Probes for Btk Occupancy Assays.

Qiu H, Caldwell R, Liu-Bujalski L, Goutopoulos A, Jones R, Potnick J, Sherer B, Bender A, Grenningloh R, Xu D, Gardberg A, Mochalkin I, Johnson T, Viacava Follis A, Head J, Morandi F.

ChemMedChem. 2019 Jan 22;14(2):217-223. doi: 10.1002/cmdc.201800714. Epub 2019 Jan 9.

PMID:
30521698
5.

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.

Bioorg Med Chem Lett. 2018 Nov 15;28(21):3419-3424. doi: 10.1016/j.bmcl.2018.09.033. Epub 2018 Sep 27.

PMID:
30290988
6.

Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors.

Qiu H, Liu-Bujalski L, Caldwell RD, Viacava Follis A, Gardberg A, Goutopoulos A, Grenningloh R, Head J, Johnson T, Jones CCV, Jones R, Mochalkin I, Morandi F, Neagu C, Potnick J, Sherer B.

Bioorg Med Chem Lett. 2018 Nov 1;28(20):3307-3311. doi: 10.1016/j.bmcl.2018.09.018. Epub 2018 Sep 15.

PMID:
30243592
7.

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.

Bioorg Med Chem Lett. 2018 Sep 15;28(17):2939-2944. doi: 10.1016/j.bmcl.2018.07.008. Epub 2018 Jul 5.

PMID:
30122225
8.

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.

Mol Pharmacol. 2017 Mar;91(3):208-219. doi: 10.1124/mol.116.107037. Epub 2017 Jan 6.

PMID:
28062735
9.

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.

Clin Immunol. 2016 Mar;164:65-77. doi: 10.1016/j.clim.2016.01.012. Epub 2016 Jan 25.

10.

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.

Front Immunol. 2014 May 22;5:233. doi: 10.3389/fimmu.2014.00233. eCollection 2014.

11.

Ets-1 facilitates nuclear entry of NFAT proteins and their recruitment to the IL-2 promoter.

Tsao HW, Tai TS, Tseng W, Chang HH, Grenningloh R, Miaw SC, Ho IC.

Proc Natl Acad Sci U S A. 2013 Sep 24;110(39):15776-81. doi: 10.1073/pnas.1304343110. Epub 2013 Sep 9.

12.

Interaction of Ets-1 with HDAC1 represses IL-10 expression in Th1 cells.

Lee CG, Kwon HK, Sahoo A, Hwang W, So JS, Hwang JS, Chae CS, Kim GC, Kim JE, So HS, Hwang ES, Grenningloh R, Ho IC, Im SH.

J Immunol. 2012 Mar 1;188(5):2244-53. doi: 10.4049/jimmunol.1101614. Epub 2012 Jan 20. Erratum in: J Immunol. 2012 Dec 15;189(12):5996.

13.

Ets-1 maintains IL-7 receptor expression in peripheral T cells.

Grenningloh R, Tai TS, Frahm N, Hongo TC, Chicoine AT, Brander C, Kaufmann DE, Ho IC.

J Immunol. 2011 Jan 15;186(2):969-76. doi: 10.4049/jimmunol.1002099. Epub 2010 Dec 10.

14.

SUMOylation attenuates c-Maf-dependent IL-4 expression.

Lin BS, Tsai PY, Hsieh WY, Tsao HW, Liu MW, Grenningloh R, Wang LF, Ho IC, Miaw SC.

Eur J Immunol. 2010 Apr;40(4):1174-84. doi: 10.1002/eji.200939788.

15.

Phylogenetic and functional analysis identifies Ets-1 as a novel regulator of the Th2 cytokine gene locus.

Strempel JM, Grenningloh R, Ho IC, Vercelli D.

J Immunol. 2010 Feb 1;184(3):1309-16. doi: 10.4049/jimmunol.0804162. Epub 2009 Dec 28.

16.

The transcription factor Ets1 is important for CD4 repression and Runx3 up-regulation during CD8 T cell differentiation in the thymus.

Zamisch M, Tian L, Grenningloh R, Xiong Y, Wildt KF, Ehlers M, Ho IC, Bosselut R.

J Exp Med. 2009 Nov 23;206(12):2685-99. doi: 10.1084/jem.20092024. Epub 2009 Nov 16.

17.

Role of Ets-1 phosphorylation in the effector function of Th cells.

Grenningloh R, Miaw SC, Moisan J, Graves BJ, Ho IC.

Eur J Immunol. 2008 Jun;38(6):1700-5. doi: 10.1002/eji.200738112.

18.

Liposome-encapsulated antigens induce a protective CTL response against Listeria monocytogenes independent of CD4+ T cell help.

Grenningloh R, Darj A, Bauer H, zur Lage S, Chakraborty T, Jacobs T, Weiss S.

Scand J Immunol. 2008 Jun;67(6):594-602. doi: 10.1111/j.1365-3083.2008.02112.x. Epub 2008 Apr 21.

19.

Ets-1 is a negative regulator of Th17 differentiation.

Moisan J, Grenningloh R, Bettelli E, Oukka M, Ho IC.

J Exp Med. 2007 Nov 26;204(12):2825-35. Epub 2007 Oct 29.

20.

Cutting Edge: Inhibition of the retinoid X receptor (RXR) blocks T helper 2 differentiation and prevents allergic lung inflammation.

Grenningloh R, Gho A, di Lucia P, Klaus M, Bollag W, Ho IC, Sinigaglia F, Panina-Bordignon P.

J Immunol. 2006 May 1;176(9):5161-6.

21.

Cysteinyl leukotrienes regulate Th2 cell-dependent pulmonary inflammation.

Kim DC, Hsu FI, Barrett NA, Friend DS, Grenningloh R, Ho IC, Al-Garawi A, Lora JM, Lam BK, Austen KF, Kanaoka Y.

J Immunol. 2006 Apr 1;176(7):4440-8.

22.

Efficient recruitment of lymphocytes in inflamed brain venules requires expression of cutaneous lymphocyte antigen and fucosyltransferase-VII.

Piccio L, Rossi B, Colantonio L, Grenningloh R, Gho A, Ottoboni L, Homeister JW, Scarpini E, Martinello M, Laudanna C, D'Ambrosio D, Lowe JB, Constantin G.

J Immunol. 2005 May 1;174(9):5805-13.

23.

Ets-1, a functional cofactor of T-bet, is essential for Th1 inflammatory responses.

Grenningloh R, Kang BY, Ho IC.

J Exp Med. 2005 Feb 21;201(4):615-26.

24.

Human dendritic cells infected by Listeria monocytogenes: induction of maturation, requirements for phagolysosomal escape and antigen presentation capacity.

Paschen A, Dittmar KE, Grenningloh R, Rohde M, Schadendorf D, Domann E, Chakraborty T, Weiss S.

Eur J Immunol. 2000 Dec;30(12):3447-56.

25.

Listeriolysin and IrpA are major protein targets of the human humoral response against Listeria monocytogenes.

Grenningloh R, Darji A, Wehland J, Chakraborty T, Weiss S.

Infect Immun. 1997 Sep;65(9):3976-80.

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