Piha-Paul SA, Hierro C, Funk JO, Gourlay SG, Smith PF, Venetsanakos E, Meric-Bernstam F, Tabernero J. A phase 1, multicenter, dose-escalation Study of PRN1371, an irreversible covalent FGFR1-4 kinase inhibitor, in patients with advanced solid tumors, followed by expansion cohorts in patients with FGFR genetic alterations. Presented at 2016 American Society of Clinical Oncology (ASCO) Annual Meeting, Chicago, IL, June 2016
Venetsanakos E, Bradshaw JM, Goldstein DM, Leung K, Karr D, Gerritsen ME, Xing Y, LaStant J, Nunn PA, Shu J, Bommireddi A, Gourlay SG, Funk JO, Brameld KA. PRN1371, an irreversible, covalent inhibitor of FGFR1, 2, 3 and 4 is highly efficacious in preclinical tumor models. Presented at American Association for Cancer Research Annual Meeting, New Orleans, LA, April 2016
Outerbridge C, Goodale E, Varjonen K, Borjesson D, Murrell D, Bisconte A, Hill R, Masjedizadeh M, Gourlay SG, White S. A New Treatment for Autoimmune Blistering Diseases: Efficacy of the Bruton's Tyrosine Kinase (BTK) Inhibitor PRN473 in Canine Pemphigus Foliaceus. Presented at AAD 2016, Washington, DC, March 5, 2016
Murrell DF, Gourlay SG, Hill RJ, Bisconte A, Francesco M, Smith P, Karr D, Outerbridge C, Varjonen K, Goodale EC, Borjesson D, Werth VP, Nunn PA, White SD. Development of PRN1008, a novel, reversible covalent BTK inhibitor in clinical development for pemphigus. Presented at Medicinal Dermatology Society Annual Meeting, Washington, DC, March 3, 2016
Smith PF, Krishnarajah, Nunn PA, Hill RJ, Karr D, Tam D, Masjedizadeh M, Gourlay SG. 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. Presented at EULAR 2015, Rome, June 13, 2015
Hill RJ, Bradshaw JM, Bisconte A, Tam D, Owens TD, Brameld KA, Smith PF, Funk JO, Goldstein DM, Nunn PA. Preclinical Characterization of PRN1008, A Novel Reversible Covalent Inhibitor of BTK That Shows Efficacy In A Rat Model of Collagen-Induced Arthritis. Presented at EULAR 2015, Rome, June 11, 2015
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. Prolonged and tunable residence time using reversible covalent kinase inhibitors. Nat. Chem Biol, 2015; May 25
Bisconte A, Hil RJ, Bradshaw JM, Verner E, Karr D, Finkle D, Brameld KA, Funk JO, Goldstein DM, Nunn PA. 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. Presented at The American Association of Immunologist Annual Meeting, New Orleans, LA, May 8-12, 2015
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. Targeting Interleukin-2-inducible T-cell Kinase (ITK) and Resting Lymphocyte Kinase (RLK) Using a Novel Covalent Inhibitor PRN694. J Biol Chem 2015 Jan 15
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. Irreversible covalent pan-FGFR Inhibitors are highly efficacious against FGFR-dependent cancers. Presented at EORTC-NCI-AACR 2014, Barcelona, November 18-21, 2014
Smith PF, Karr D, Bisconte A, Hill RJ Goldstein DM Nunn PA, Funk JO. Development of a Disease Model of Bruton's Tyrosine Kinase (BTK) Inhibition by PRN473 in Rat Collagen-Induced Arthritis (rCIA). Presented at American Conference on Pharmacometrics, Las Vegas, NV October 12-15, 2014
Hill RJ, Bisconte A, Bradshaw JM, Brameld K, Kim EO, Li X, et al. Discovery of a highly potent, selective reversible covalent inhibitor of JAK3 kinase [abstract]. Arthritis Rheum 2012;64 Suppl 10:2326.
Serafimova IM, Pufall MA, Krishnan S, Duda K, Cohen MS, Maglathlin RL, McFarland JM, Miller RM, Frödin M, Taunton J. Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles. Nat Chem Biol, 2012; Apr 1:8(5):471-6.