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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: follis av. 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
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: follis av. 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
Regulation of apoptosis by an intrinsically disordered region of Bcl-xL.
Follis AV, Llambi F, Kalkavan H, Yao Y, Phillips AH, Park CG, Marassi FM, Green DR, Kriwacki RW. Follis AV, et al. Nat Chem Biol. 2018 May;14(5):458-465. doi: 10.1038/s41589-018-0011-x. Epub 2018 Mar 5. Nat Chem Biol. 2018. PMID: 29507390 Free PMC article.
Many players in BCL-2 family affairs.
Moldoveanu T, Follis AV, Kriwacki RW, Green DR. Moldoveanu T, et al. Among authors: follis av. Trends Biochem Sci. 2014 Mar;39(3):101-11. doi: 10.1016/j.tibs.2013.12.006. Epub 2014 Feb 3. Trends Biochem Sci. 2014. PMID: 24503222 Free PMC article. Review.
17 results