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The Interleukin-1 Receptor-Associated Kinase 4 Inhibitor PF-06650833 Blocks Inflammation in Preclinical Models of Rheumatic Disease and in Humans Enrolled in a Randomized Clinical Trial.
Winkler A, Sun W, De S, Jiao A, Sharif MN, Symanowicz PT, Athale S, Shin JH, Wang J, Jacobson BA, Ramsey SJ, Dower K, Andreyeva T, Liu H, Hegen M, Homer BL, Brodfuehrer J, Tilley M, Gilbert SA, Danto SI, Beebe JJ, Barnes BJ, Pascual V, Lin LL, Kilty I, Fleming M, Rao VR. Winkler A, et al. Among authors: kilty i. Arthritis Rheumatol. 2021 Dec;73(12):2206-2218. doi: 10.1002/art.41953. Epub 2021 Nov 1. Arthritis Rheumatol. 2021. PMID: 34423919 Free PMC article. Clinical Trial.
Safety, tolerability, pharmacokinetics, and pharmacodynamics of PF-06650833, a selective interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, in single and multiple ascending dose randomized phase 1 studies in healthy subjects.
Danto SI, Shojaee N, Singh RSP, Li C, Gilbert SA, Manukyan Z, Kilty I. Danto SI, et al. Among authors: kilty i. Arthritis Res Ther. 2019 Dec 5;21(1):269. doi: 10.1186/s13075-019-2008-6. Arthritis Res Ther. 2019. PMID: 31805989 Free PMC article. Clinical Trial.
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: kilty ic. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor.
Xu H, Jesson MI, Seneviratne UI, Lin TH, Sharif MN, Xue L, Nguyen C, Everley RA, Trujillo JI, Johnson DS, Point GR, Thorarensen A, Kilty I, Telliez JB. Xu H, et al. Among authors: kilty i. ACS Chem Biol. 2019 Jun 21;14(6):1235-1242. doi: 10.1021/acschembio.9b00188. Epub 2019 May 22. ACS Chem Biol. 2019. PMID: 31082193
Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin.
Jones P, Storer RI, Sabnis YA, Wakenhut FM, Whitlock GA, England KS, Mukaiyama T, Dehnhardt CM, Coe JW, Kortum SW, Chrencik JE, Brown DG, Jones RM, Murphy JR, Yeoh T, Morgan P, Kilty I. Jones P, et al. Among authors: kilty i. J Med Chem. 2017 Jan 26;60(2):767-786. doi: 10.1021/acs.jmedchem.6b01634. Epub 2017 Jan 4. J Med Chem. 2017. PMID: 27983835
TAK1 inhibition in the DFG-out conformation.
Kilty I, Green MP, Bell AS, Brown DG, Dodd PG, Hewson C, Hughes SJ, Phillips C, Ryckmans T, Smith RT, van Hoorn WP, Cohen P, Jones LH. Kilty I, et al. Chem Biol Drug Des. 2013 Nov;82(5):500-5. doi: 10.1111/cbdd.12169. Chem Biol Drug Des. 2013. PMID: 23745990
Glycogen synthase kinase-3β modulation of glucocorticoid responsiveness in COPD.
Ngkelo A, Hoffmann RF, Durham AL, Marwick JA, Brandenburg SM, de Bruin HG, Jonker MR, Rossios C, Tsitsiou E, Caramori G, Contoli M, Casolari P, Monaco F, Andò F, Speciale G, Kilty I, Chung KF, Papi A, Lindsay MA, Ten Hacken NH, van den Berge M, Timens W, Barnes PJ, van Oosterhout AJ, Adcock IM, Kirkham PA, Heijink IH. Ngkelo A, et al. Among authors: kilty i. Am J Physiol Lung Cell Mol Physiol. 2015 Nov 15;309(10):L1112-23. doi: 10.1152/ajplung.00077.2015. Epub 2015 Aug 28. Am J Physiol Lung Cell Mol Physiol. 2015. PMID: 26320152 Free PMC article.
44 results