Targeting Interleukin-2-inducible T-cell Kinase (ITK) and Resting Lymphocyte Kinase (RLK) Using a Novel Covalent Inhibitor PRN694

Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors

(2014) Seungil Han et al.   BIOCHEMICAL JOURNAL

Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors

(2014) Richard M. Pastor et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Itk-mediated integration of T cell receptor and cytokine signaling regulates the balance between Th17 and regulatory T cells

(2014) Julio Gomez-Rodriguez et al.   JOURNAL OF EXPERIMENTAL MEDICINE

The Tec Kinases Itk and Rlk Regulate NKT Cell Maturation, Cytokine Production, and Survival

(2014) M. Felices et al.   JOURNAL OF IMMUNOLOGY

Surface CD107a/LAMP-1 protects natural killer cells from degranulation-associated damage

(2013) A. Cohnen et al.   BLOOD

Ibrutinib is an irreversible molecular inhibitor of ITK driving a Th1-selective pressure in T lymphocytes

(2013) J. A. Dubovsky et al.   BLOOD

Th17 Cells in Immunity and Autoimmunity

(2013) Simone Kennedy Bedoya et al.   Clinical & Developmental Immunology

Models for mature T-cell lymphomas—A critical appraisal of experimental systems and their contribution to current T-cell tumorigenic concepts

(2013) Kathrin Warner et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Discovery of Novel Irreversible Inhibitors of Interleukin (IL)-2-inducible Tyrosine Kinase (Itk) by Targeting Cysteine 442 in the ATP Pocket

(2013) John D. Harling et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting BTK with Ibrutinib in Relapsed or Refractory Mantle-Cell Lymphoma

(2013) Michael L. Wang et al.   NEW ENGLAND JOURNAL OF MEDICINE

Targeting BTK with Ibrutinib in Relapsed Chronic Lymphocytic Leukemia

(2013) John C. Byrd et al.   NEW ENGLAND JOURNAL OF MEDICINE

Regulation of IL-17A Production Is Distinct from IL-17F in a Primary Human Cell Co-culture Model of T Cell-Mediated B Cell Activation

(2013) Andrew C. Melton et al.   PLoS One

The Tyrosine Kinase Btk Regulates the Macrophage Response to Listeria monocytogenes Infection

(2013) Afitap Derya Köprülü et al.   PLoS One

Inhibitors of BTK and ITK: State of the New Drugs for Cancer, Autoimmunity and Inflammatory Diseases

(2013) L. Vargas et al.   SCANDINAVIAN JOURNAL OF IMMUNOLOGY

Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy

(2013) Catherine M. Alder et al.   ACS Medicinal Chemistry Letters

T-Cell Receptor Signaling in Peripheral T-Cell Lymphoma – A Review of Patterns of Alterations in a Central Growth Regulatory Pathway

(2013) Kathrin Warner et al.   Current Hematologic Malignancy Reports

X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase

(2012) Larry R. McLean et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Tec Family Kinases in Inflammation and Disease

(2012) Nicole J. Horwood et al.   INTERNATIONAL REVIEWS OF IMMUNOLOGY

Reversible targeting of noncatalytic cysteines with chemically tuned electrophiles

(2012) Iana M Serafimova et al.   Nature Chemical Biology

A selective inhibitor reveals PI3Kγ dependence of TH17 cell differentiation

(2012) Giovanna Bergamini et al.   Nature Chemical Biology

Brodalumab, an Anti–Interleukin-17–Receptor Antibody for Psoriasis

(2012) Kim A. Papp et al.   NEW ENGLAND JOURNAL OF MEDICINE

Functional relevance of T helper 17 (Th17) cells and the IL-17 cytokine family in inflammatory bowel disease

(2011) Gheorghe Hundorfean et al.   INFLAMMATORY BOWEL DISEASES

Absence of Tec Family Kinases Interleukin-2 Inducible T cell Kinase (Itk) and Bruton's Tyrosine Kinase (Btk) Severely Impairs FcϵRI-dependent Mast Cell Responses

(2011) Archana S. Iyer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery and Structure−Activity Relationship of 3-Aminopyrid-2-ones as Potent and Selective Interleukin-2 Inducible T-Cell Kinase (Itk) Inhibitors

(2011) Jean-Damien Charrier et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effect of increased HoxB4 on human megakaryocytic development

(2010) Yiming Zhong et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK)

(2010) Avdhoot D. Velankar et al.   BIOORGANIC & MEDICINAL CHEMISTRY

T-Cell Signaling Regulated by the Tec Family Kinase, Itk

(2010) A. H. Andreotti et al.   Cold Spring Harbor Perspectives in Biology

Frequency and phenotype of peripheral blood Th17 cells in ankylosing spondylitis and rheumatoid arthritis

(2009) Hui Shen et al.   ARTHRITIS AND RHEUMATISM

Treatment of Chronic Lymphocytic Leukemia with a Hypomethylating Agent Induces Expression of NXF2, an Immunogenic Cancer Testis Antigen

(2009) J. A. Dubovsky et al.   CLINICAL CANCER RESEARCH

ITK Inhibitors in Inflammation and Immune-Mediated Disorders

(2009) Nisebita Sahu et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Crohn's disease: Th1, Th17 or both? The change of a paradigm: new immunological and genetic insights implicate Th17 cells in the pathogenesis of Crohn's disease

(2009) S. Brand   GUT

Differential Expression of Interleukin-17A and -17F Is Coupled to T Cell Receptor Signaling via Inducible T Cell Kinase

(2009) Julio Gomez-Rodriguez et al.   IMMUNITY

Tec kinases regulate T-lymphocyte development and function: new insights into the roles of Itk and Rlk/Txk

(2009) Julie A. Readinger et al.   IMMUNOLOGICAL REVIEWS

Tec protein tyrosine kinase inhibits CD25 expression in human T-lymphocyte

(2009) Kentaro Susaki et al.   IMMUNOLOGY LETTERS

Targeted therapy in T-cell malignancies: dysregulation of the cellular signaling pathways

(2009) W-L Zhao   LEUKEMIA

Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk)

(2008) Kevin J. Moriarty et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Lenalidomide Enhances Natural Killer Cell and Monocyte-Mediated Antibody-Dependent Cellular Cytotoxicity of Rituximab-Treated CD20+ Tumor Cells

(2008) L. Wu et al.   CLINICAL CANCER RESEARCH

IL23 differentially regulates the Th1/Th17 balance in ulcerative colitis and Crohn's disease

(2008) T Kobayashi et al.   GUT

Psoriasis Vulgaris Lesions Contain Discrete Populations of Th1 and Th17 T Cells

(2008) Michelle A. Lowes et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Psoriasis Is Characterized by Accumulation of Immunostimulatory and Th1/Th17 Cell-Polarizing Myeloid Dendritic Cells

(2008) Lisa C. Zaba et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY