Proteins > Tyrosine-protein kinase ITK/TSK
Page last updated: 2024-08-07 17:03:04
Tyrosine-protein kinase ITK/TSK
A tyrosine-protein kinase ITK/TSK that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q08881]
Synonyms
EC 2.7.10.2;
Interleukin-2-inducible T-cell kinase;
IL-2-inducible T-cell kinase;
Kinase EMT;
T-cell-specific kinase;
Tyrosine-protein kinase Lyk
Research
Bioassay Publications (36)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 15 (41.67) | 29.6817 |
| 2010's | 11 (30.56) | 24.3611 |
| 2020's | 10 (27.78) | 2.80 |
Compounds (86)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Discovery and optimization of selective FGFR4 inhibitors via scaffold hopping.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Crystal structures of interleukin-2 tyrosine kinase and their implications for the design of selective inhibitors.The Journal of biological chemistry, , Apr-30, Volume: 279, Issue:18, 2004
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 18, Issue:22, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent.Journal of medicinal chemistry, , Mar-25, Volume: 47, Issue:7, 2004
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor.ACS medicinal chemistry letters, , Oct-13, Volume: 2, Issue:10, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.Proceedings of the National Academy of Sciences of the United States of America, , Aug-14, Volume: 104, Issue:33, 2007
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities.Journal of medicinal chemistry, , Aug-29, Volume: 45, Issue:18, 2002
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.ACS chemical biology, , 12-16, Volume: 11, Issue:12, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 16, Issue:14, 2006
Features of selective kinase inhibitors.Chemistry & biology, , Volume: 12, Issue:6, 2005
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580.Proceedings of the National Academy of Sciences of the United States of America, , Nov-01, Volume: 102, Issue:44, 2005
Ophiorrhines F and G, Key Biogenetic Intermediates of Ophiorrhine Alkaloids from Journal of natural products, , 02-25, Volume: 85, Issue:2, 2022
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
[no title available]Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Review of the development of BTK inhibitors in overcoming the clinical limitations of ibrutinib.European journal of medicinal chemistry, , Feb-05, Volume: 229, 2022
Discovery of 1-Amino-1Journal of medicinal chemistry, , 11-11, Volume: 64, Issue:21, 2021
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold.European journal of medicinal chemistry, , Aug-01, Volume: 199, 2020
Discovery of quinoline-based irreversible BTK inhibitors.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 30, Issue:14, 2020
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Discovery and biological evaluation of N5-substituted 6,7-dioxo-6,7-dihydropteridine derivatives as potent Bruton's tyrosine kinase inhibitors.MedChemComm, , Apr-01, Volume: 9, Issue:4, 2018
[no title available]European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Discovery of 4,7-Diamino-5-(4-phenoxyphenyl)-6-methylene-pyrimido[5,4- b]pyrrolizines as Novel Bruton's Tyrosine Kinase Inhibitors.Journal of medicinal chemistry, , 05-24, Volume: 61, Issue:10, 2018
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
The Ascension of Targeted Covalent Inhibitors.Journal of medicinal chemistry, , 04-28, Volume: 65, Issue:8, 2022
Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Discovery of 1-Amino-1Journal of medicinal chemistry, , 11-11, Volume: 64, Issue:21, 2021
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of quinoline-based irreversible BTK inhibitors.Bioorganic & medicinal chemistry letters, , 07-15, Volume: 30, Issue:14, 2020
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| non-membrane spanning protein tyrosine kinase activity | molecular function | Catalysis of the reaction: ATP + protein L-tyrosine = ADP + protein L-tyrosine phosphate by a non-membrane spanning protein. [EC:2.7.10.2] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
| cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
| cell-cell junction | cellular component | A cell junction that forms a connection between two or more cells of an organism; excludes direct cytoplasmic intercellular bridges, such as ring canals in insects. [GOC:aruk, GOC:bc, GOC:dgh, GOC:hb, GOC:mah, PMID:21422226, PMID:28096264] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 12 target(s):
| Target | Category | Definition |
|---|
| positive regulation of cytokine production | biological process | Any process that activates or increases the frequency, rate or extent of production of a cytokine. [GOC:add, ISBN:0781735149] |
| adaptive immune response | biological process | An immune response mediated by cells expressing specific receptors for antigens produced through a somatic diversification process, and allowing for an enhanced secondary response to subsequent exposures to the same antigen (immunological memory). [GO_REF:0000022, GOC:add, ISBN:0781735149] |
| cellular defense response | biological process | A defense response that is mediated by cells. [GOC:ebc] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| activation of phospholipase C activity | biological process | The initiation of the activity of the inactive enzyme phospolipase C as the result of The series of molecular signals generated as a consequence of a G protein-coupled receptor binding to its physiological ligand. [GOC:dph, GOC:mah, GOC:tb, PMID:8280098] |
| intracellular signal transduction | biological process | The process in which a signal is passed on to downstream components within the cell, which become activated themselves to further propagate the signal and finally trigger a change in the function or state of the cell. [GOC:bf, GOC:jl, GOC:signaling, ISBN:3527303782] |
| T cell activation | biological process | The change in morphology and behavior of a mature or immature T cell resulting from exposure to a mitogen, cytokine, chemokine, cellular ligand, or an antigen for which it is specific. [GOC:mgi_curators, ISBN:0781735149] |
| gamma-delta T cell activation | biological process | The change in morphology and behavior of a gamma-delta T cell resulting from exposure to a mitogen, cytokine, chemokine, cellular ligand, or an antigen for which it is specific. [GOC:add] |
| T cell receptor signaling pathway | biological process | The series of molecular signals initiated by the cross-linking of an antigen receptor on a T cell. [GOC:add] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| B cell receptor signaling pathway | biological process | The series of molecular signals initiated by the cross-linking of an antigen receptor on a B cell. [GOC:add] |
| NK T cell differentiation | biological process | The process in which a precursor cell type acquires the specialized features of a NK T cell. [GOC:add, ISBN:0781735149, PMID:10704459] |