June 2015
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A Phase 1 Clinical Trial of PRN1008, An Oral, Reversible, Covalent BTK Inhibitor Demonstrates Clinical Safety and Therapeutic Levels of BTK Occupancy Without Sustained Systemic Exposure
Smith PF, Krishnarajah, Nunn PA, Hill RJ, Karr D, Tam D, Masjedizadeh M, Gourlay SG.
Presented at EULAR 2015, Rome, June 13, 2015
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June 2015
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Preclinical Characterization of PRN1008, A Novel Reversible Covalent Inhibitor of BTK That Shows Efficacy In A Rat Model of Collagen-Induced Arthritis
Hill RJ, Bradshaw JM, Bisconte A, Tam D, Owens TD, Brameld KA, Smith PF, Funk JO, Goldstein DM, Nunn PA.
Presented at EULAR 2015, Rome, June 11, 2015
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May 2015
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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.
Nat. Chem Biol, 2015; May 25
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May 2015
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Efficacy in collagen induced arthritis models with a selective, reversible covalent Bruton’s Tyrosine Kinase (BTK) inhibitor PRN473 is driven by durable target occupancy rather than extended plasma exposure
Bisconte A, Hil RJ, Bradshaw JM, Verner E, Karr D, Finkle D, Brameld KA, Funk JO, Goldstein DM, Nunn PA.
Presented at The American Association of Immunologist Annual Meeting, New Orleans, LA, May 8-12, 2015
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January 2015
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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.
J Biol Chem 2015 Jan 15
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November 2014
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Irreversible covalent pan-FGFR Inhibitors are highly efficacious against FGFR-dependent cancers.
Phan VT, Verner E, Gerritsen M, Bradshaw JM, Goldstein DM, Hill RJ, Karr D, LaStant J, Nunn P, Tam D, Shu J, Funk JO, Brameld KA.
Presented at EORTC-NCI-AACR 2014, Barcelona, November 18-21, 2014
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November 2014
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Development of a Disease Model of Bruton’s Tyrosine Kinase (BTK) Inhibition by PRN473 in Rat Collagen-Induced Arthritis (rCIA)
Smith PF, Karr D, Bisconte A, Hill RJ Goldstein DM Nunn PA, Funk JO.
Presented at American Conference on Pharmacometrics, Las Vegas, NV October 12-15, 2014
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May 2012
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Discovery of a highly potent, selective reversible covalent inhibitor of JAK3 kinase [abstract]
Hill RJ, Bisconte A, Bradshaw JM, Brameld K, Kim EO, Li X, et al.
Arthritis Rheum 2012;64 Suppl 10:2326
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