Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain

Structure of the pseudokinase-kinase domains from protein kinase TYK2 reveals a mechanism for Janus kinase (JAK) autoinhibition

(2014) P. J. Lupardus et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Activating Janus kinase pseudokinase domain mutations in myeloproliferative and other blood cancers

(2013) Stefan N. Constantinescu et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

Lead Optimization of a 4-Aminopyridine Benzamide Scaffold To Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors

(2013) Jun Liang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure of a pseudokinase-domain switch that controls oncogenic activation of Jak kinases

(2013) Angela V Toms et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Randomized Phase 2b Trial of Tofacitinib (CP-690,550) in De Novo Kidney Transplant Patients: Efficacy, Renal Function and Safety at 1 Year

(2012) F. Vincenti et al.   AMERICAN JOURNAL OF TRANSPLANTATION

Selective JAK1 inhibitor and selective Tyk2 inhibitor patents

(2012) Peter Norman   EXPERT OPINION ON THERAPEUTIC PATENTS

Targeting IL-17 and TH17 cells in chronic inflammation

(2012) Pierre Miossec et al.   NATURE REVIEWS DRUG DISCOVERY

Crystal structures of the JAK2 pseudokinase domain and the pathogenic mutant V617F

(2012) Rajintha M Bandaranayake et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Ustekinumab Induction and Maintenance Therapy in Refractory Crohn's Disease

(2012) William J. Sandborn et al.   NEW ENGLAND JOURNAL OF MEDICINE

REFMAC5 for the refinement of macromolecular crystal structures

(2011) Garib N. Murshudov et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Tyrosine kinase 2 variant influences T lymphocyte polarization and multiple sclerosis susceptibility

(2011) N. Couturier et al.   BRAIN

Efficacy and safety results from a phase III, randomized controlled trial comparing the safety and efficacy of briakinumab with etanercept and placebo in patients with moderate to severe chronic plaque psoriasis

(2011) B.E. Strober et al.   BRITISH JOURNAL OF DERMATOLOGY

IL-23–responsive innate lymphoid cells are increased in inflammatory bowel disease

(2011) Alessandra Geremia et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Characterization of BMS-911543, a functionally selective small-molecule inhibitor of JAK2

(2011) A V Purandare et al.   LEUKEMIA

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Pseudokinases-remnants of evolution or key allosteric regulators?

(2010) Elton Zeqiraj et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Trends in Kinase Selectivity: Insights for Target Class-Focused Library Screening

(2010) Shana L. Posy et al.   JOURNAL OF MEDICINAL CHEMISTRY

A phase 2, 24-week, randomized, placebo-controlled, double-blind study examining the efficacy and safety of an anti-interleukin-12 and -23 monoclonal antibody in patients with relapsing–remitting or secondary progressive multiple sclerosis

(2010) Timothy L Vollmer et al.   Multiple Sclerosis Journal

Replication analysis identifies TYK2 as a multiple sclerosis susceptibility factor

(2009) Maria Ban et al.   EUROPEAN JOURNAL OF HUMAN GENETICS

Why did IL-12/IL-23 antibody therapy fail in multiple sclerosis?

(2009) Erin E Longbrake et al.   Expert Review of Neurotherapeutics

The JAK2V617 mutation induces constitutive activation and agonist hypersensitivity in basophils from patients with polycythemia vera

(2009) L. Pieri et al.   HAEMATOLOGICA

Tyrosine Kinase 2 Plays Critical Roles in the Pathogenic CD4 T Cell Responses for the Development of Experimental Autoimmune Encephalomyelitis

(2009) A. Oyamada et al.   JOURNAL OF IMMUNOLOGY

Novel Tricyclic Inhibitors of IκB Kinase

(2009) James Kempson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Periodic, Partial Inhibition of I B Kinase  -Mediated Signaling Yields Therapeutic Benefit in Preclinical Models of Rheumatoid Arthritis

(2009) K. M. Gillooly et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Do enthalpy and entropy distinguish first in class from best in class?

(2008) E FREIRE   DRUG DISCOVERY TODAY

Differential Regulation of STAT Family Members by Glycogen Synthase Kinase-3

(2008) Eléonore Beurel et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A critical function for transforming growth factor-β, interleukin 23 and proinflammatory cytokines in driving and modulating human TH-17 responses

(2008) Elisabetta Volpe et al.   NATURE IMMUNOLOGY