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Page 1
Activation mechanism and steady state kinetics of Bruton's tyrosine kinase.
Dinh M, Grunberger D, Ho H, Tsing SY, Shaw D, Lee S, Barnett J, Hill RJ, Swinney DC, Bradshaw JM. Dinh M, et al. Among authors: hill rj. J Biol Chem. 2007 Mar 23;282(12):8768-76. doi: 10.1074/jbc.M609920200. Epub 2007 Jan 30. J Biol Chem. 2007. PMID: 17264076 Free article.
3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: design and development to a highly selective lead.
Soth M, Abbot S, Abubakari A, Arora N, Arzeno H, Billedeau R, Dewdney N, Durkin K, Frauchiger S, Ghate M, Goldstein DM, Hill RJ, Kuglstatter A, Li F, Loe B, McCaleb K, McIntosh J, Papp E, Park J, Stahl M, Sung ML, Suttman R, Swinney DC, Weller P, Wong B, Zecic H, Gabriel T. Soth M, et al. Among authors: hill rj. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3452-6. doi: 10.1016/j.bmcl.2011.03.098. Epub 2011 Apr 1. Bioorg Med Chem Lett. 2011. PMID: 21515047
Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694.
Zhong Y, Dong S, Strattan E, Ren L, Butchar JP, Thornton K, Mishra A, Porcu P, Bradshaw JM, Bisconte A, Owens TD, Verner E, Brameld KA, Funk JO, Hill RJ, Johnson AJ, Dubovsky JA. Zhong Y, et al. Among authors: hill rj. J Biol Chem. 2015 Mar 6;290(10):5960-78. doi: 10.1074/jbc.M114.614891. Epub 2015 Jan 15. J Biol Chem. 2015. PMID: 25593320 Free PMC article.
Discovery of Reversible Covalent Bruton's Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib).
Owens TD, Brameld KA, Verner EJ, Ton T, Li X, Zhu J, Masjedizadeh MR, Bradshaw JM, Hill RJ, Tam D, Bisconte A, Kim EO, Francesco M, Xing Y, Shu J, Karr D, LaStant J, Finkle D, Loewenstein N, Haberstock-Debic H, Taylor MJ, Nunn P, Langrish CL, Goldstein DM. Owens TD, et al. Among authors: hill rj. J Med Chem. 2022 Apr 14;65(7):5300-5316. doi: 10.1021/acs.jmedchem.1c01170. Epub 2022 Mar 18. J Med Chem. 2022. PMID: 35302767
The kinase activities of interleukin-1 receptor associated kinase (IRAK)-1 and 4 are redundant in the control of inflammatory cytokine expression in human cells.
Song KW, Talamas FX, Suttmann RT, Olson PS, Barnett JW, Lee SW, Thompson KD, Jin S, Hekmat-Nejad M, Cai TZ, Manning AM, Hill RJ, Wong BR. Song KW, et al. Among authors: hill rj. Mol Immunol. 2009 Apr;46(7):1458-66. doi: 10.1016/j.molimm.2008.12.012. Epub 2009 Jan 31. Mol Immunol. 2009. PMID: 19181383
Preclinical Efficacy and Anti-Inflammatory Mechanisms of Action of the Bruton Tyrosine Kinase Inhibitor Rilzabrutinib for Immune-Mediated Disease.
Langrish CL, Bradshaw JM, Francesco MR, Owens TD, Xing Y, Shu J, LaStant J, Bisconte A, Outerbridge C, White SD, Hill RJ, Brameld KA, Goldstein DM, Nunn PA. Langrish CL, et al. Among authors: hill rj. J Immunol. 2021 Apr 1;206(7):1454-1468. doi: 10.4049/jimmunol.2001130. Epub 2021 Mar 5. J Immunol. 2021. PMID: 33674445 Free PMC article.
Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis.
Lou Y, Han X, Kuglstatter A, Kondru RK, Sweeney ZK, Soth M, McIntosh J, Litman R, Suh J, Kocer B, Davis D, Park J, Frauchiger S, Dewdney N, Zecic H, Taygerly JP, Sarma K, Hong J, Hill RJ, Gabriel T, Goldstein DM, Owens TD. Lou Y, et al. Among authors: hill rj. J Med Chem. 2015 Jan 8;58(1):512-6. doi: 10.1021/jm500305p. Epub 2014 Apr 16. J Med Chem. 2015. PMID: 24712864
Prolonged and tunable residence time using reversible covalent kinase inhibitors.
Bradshaw JM, McFarland JM, Paavilainen VO, Bisconte A, Tam D, Phan VT, Romanov S, Finkle D, Shu J, Patel V, Ton T, Li X, Loughhead DG, Nunn PA, Karr DE, Gerritsen ME, Funk JO, Owens TD, Verner E, Brameld KA, Hill RJ, Goldstein DM, Taunton J. Bradshaw JM, et al. Among authors: hill rj. Nat Chem Biol. 2015 Jul;11(7):525-31. doi: 10.1038/nchembio.1817. Epub 2015 May 25. Nat Chem Biol. 2015. PMID: 26006010 Free PMC article.
372 results