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In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II.
Revesz L, Schlapbach A, Aichholz R, Dawson J, Feifel R, Hawtin S, Littlewood-Evans A, Koch G, Kroemer M, Möbitz H, Scheufler C, Velcicky J, Huppertz C. Revesz L, et al. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4719-23. doi: 10.1016/j.bmcl.2010.04.023. Epub 2010 Apr 11. Bioorg Med Chem Lett. 2010. PMID: 20591669
Requirement of Mucosa-Associated Lymphoid Tissue Lymphoma Translocation Protein 1 Protease Activity for Fcγ Receptor-Induced Arthritis, but Not Fcγ Receptor-Mediated Platelet Elimination, in Mice.
Martin K, Touil R, Cvijetic G, Israel L, Kolb Y, Sarret S, Valeaux S, Degl'Innocenti E, Le Meur T, Caesar N, Bardet M, Beerli C, Zerwes HG, Kovarik J, Beltz K, Schlapbach A, Quancard J, Régnier CH, Bigaud M, Junt T, Wieczorek G, Isnardi I, Littlewood-Evans A, Bornancin F, Calzascia T. Martin K, et al. Arthritis Rheumatol. 2020 Jun;72(6):919-930. doi: 10.1002/art.41204. Epub 2020 Apr 26. Arthritis Rheumatol. 2020. PMID: 31943941
Nonhematopoietic IRAK1 drives arthritis via neutrophil chemoattractants.
Hoyler T, Bannert B, André C, Beck D, Boulay T, Buffet D, Caesar N, Calzascia T, Dawson J, Kyburz D, Hennze R, Huppertz C, Littlewood-Evans A, Loetscher P, Mertz KD, Niwa S, Robert G, Rush JS, Ruzzante G, Sarret S, Stein T, Touil I, Wieczorek G, Zipfel G, Hawtin S, Junt T. Hoyler T, et al. Among authors: littlewood evans a. JCI Insight. 2022 Jul 8;7(13):e149825. doi: 10.1172/jci.insight.149825. JCI Insight. 2022. PMID: 35801586 Free PMC article.
Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.
Schubart A, Anderson K, Mainolfi N, Sellner H, Ehara T, Adams CM, Mac Sweeney A, Liao SM, Crowley M, Littlewood-Evans A, Sarret S, Wieczorek G, Perrot L, Dubost V, Flandre T, Zhang Y, Smith RJH, Risitano AM, Karki RG, Zhang C, Valeur E, Sirockin F, Gerhartz B, Erbel P, Hughes N, Smith TM, Cumin F, Argikar UA, Haraldsson B, Mogi M, Sedrani R, Wiesmann C, Jaffee B, Maibaum J, Flohr S, Harrison R, Eder J. Schubart A, et al. Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7926-7931. doi: 10.1073/pnas.1820892116. Epub 2019 Mar 29. Proc Natl Acad Sci U S A. 2019. PMID: 30926668 Free PMC article.
Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.
Hoegenauer K, Soldermann N, Zécri F, Strang RS, Graveleau N, Wolf RM, Cooke NG, Smith AB, Hollingworth GJ, Blanz J, Gutmann S, Rummel G, Littlewood-Evans A, Burkhart C. Hoegenauer K, et al. ACS Med Chem Lett. 2017 Aug 25;8(9):975-980. doi: 10.1021/acsmedchemlett.7b00293. eCollection 2017 Sep 14. ACS Med Chem Lett. 2017. PMID: 28947947 Free PMC article.
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Angst D, Gessier F, Janser P, Vulpetti A, Wälchli R, Beerli C, Littlewood-Evans A, Dawson J, Nuesslein-Hildesheim B, Wieczorek G, Gutmann S, Scheufler C, Hinniger A, Zimmerlin A, Funhoff EG, Pulz R, Cenni B. Angst D, et al. Among authors: littlewood evans a. J Med Chem. 2020 May 28;63(10):5102-5118. doi: 10.1021/acs.jmedchem.9b01916. Epub 2020 Mar 4. J Med Chem. 2020. PMID: 32083858
47 results