tec protein tyrosine kinase | Tec family | IUPHAR/BPS Guide to PHARMACOLOGY

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tec protein tyrosine kinase

target has curated data in GtoImmuPdb

Target id: 2238

Nomenclature: tec protein tyrosine kinase

Abbreviated Name: TEC

Family: Tec family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 631 4p12 TEC tec protein tyrosine kinase
Mouse - 630 5 C3.2 Tec tec protein tyrosine kinase
Rat - 629 14 p11 Tec tec protein tyrosine kinase
Previous and Unofficial Names
PSCTK4
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Solution NMR structure of PH domain of tyrosine-protein kinase Tec from Homo sapiens, Northeast Structural Genomics Consortium (NESG) target HR3504C.
PDB Id:  2LUL
Resolution:  0.0Å
Species:  Human
References: 
Enzyme Reaction
EC Number: 2.7.10.2

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PRN694 Hs Inhibition 8.5 pIC50 9
pIC50 8.5 (IC50 3.3x10-9 M) [9]
compound 9 [PMID: 26006010] Hs Inhibition 8.5 pIC50 3
pIC50 8.5 (IC50 3.4x10-9 M) [3]
compound 38 [PMID: 24915291] Hs Inhibition 8.2 pIC50 7
pIC50 8.2 (IC50 6.3x10-9 M) [7]
ibrutinib Hs Inhibition 8.1 pIC50 4
pIC50 8.1 (IC50 7x10-9 M) [4]
compound 31 [PMID: 24915291] Hs Inhibition 8.1 pIC50 7
pIC50 8.1 (IC50 8.2x10-9 M) [7]
acalabrutinib Hs Inhibition 7.0 pIC50 4
pIC50 7.0 (IC50 9.3x10-8 M) [4]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 5,8

Key to terms and symbols Click column headers to sort
Target used in screen: TEC
Ligand Sp. Type Action Value Parameter
dasatinib Hs Inhibitor Inhibition 7.9 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.7 pKd
foretinib Hs Inhibitor Inhibition 6.5 pKd
PD-173955 Hs Inhibitor Inhibition 6.2 pKd
MLN-8054 Hs Inhibitor Inhibition 6.1 pKd
lestaurtinib Hs Inhibitor Inhibition 5.9 pKd
staurosporine Hs Inhibitor Inhibition 5.9 pKd
canertinib Hs Inhibitor Inhibition 5.8 pKd
tamatinib Hs Inhibitor Inhibition 5.8 pKd
JNJ-28312141 Hs Inhibitor Inhibition 5.7 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,6

Key to terms and symbols Click column headers to sort
Target used in screen: Tec (activated)/nd
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 3.0 2.0
Gö 6976 Hs Inhibitor Inhibition 4.0 9.0
Lck inhibitor Hs Inhibitor Inhibition 10.0 0.0
GSK-3 inhibitor IX Hs Inhibitor Inhibition 15.0 13.0
staurosporine Hs Inhibitor Inhibition 17.0 2.5
TWS119 Hs Inhibitor Inhibition 17.0 0.0
Cdk2 inhibitor IV Hs Inhibitor Inhibition 24.0 2.0
aloisine A Hs Inhibitor Inhibition 38.0 9.0
GSK-3 inhibitor XIII Hs Inhibitor Inhibition 38.0 4.0
CGP74514A Hs Inhibitor Inhibition 39.0 7.0
Target used in screen: nd/TEC
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 2.4
Lck inhibitor Hs Inhibitor Inhibition 8.3
dasatinib Hs Inhibitor Inhibition 11.3
Src kinase inhibitor I Hs Inhibitor Inhibition 43.3
EGFR/ErbB-2/ErbB-4 inhibitor Hs Inhibitor Inhibition 52.1
Cdk2 inhibitor IV Hs Inhibitor Inhibition 63.0
masitinib Hs Inhibitor Inhibition 83.2
K-252a Hs Inhibitor Inhibition 84.2
MNK1 inhibitor Hs Inhibitor Inhibition 86.0
MK2a inhibitor Hs Inhibitor Inhibition 86.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
The TEC family protein tyrosine kinases have been identified as key components of T-cell-receptor activation and signalling. TEC family kinases are expressed predominantly by haematopoietic cells. T cells express ITK, TXK and TEC [2].
Immuno Process Associations
Immuno Process:  Immune regulation
GO Annotations:  Associated to 3 GO processes
GO:0038095 Fc-epsilon receptor signaling pathway TAS
GO:0050852 T cell receptor signaling pathway IBA
GO:0050853 B cell receptor signaling pathway IDA
Immuno Process:  Tissue repair
GO Annotations:  Associated to 1 GO processes
GO:0042246 tissue regeneration IBA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes
GO:0019221 cytokine-mediated signaling pathway TAS
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 3 GO processes
GO:0038095 Fc-epsilon receptor signaling pathway TAS
GO:0050852 T cell receptor signaling pathway IBA
GO:0050853 B cell receptor signaling pathway IDA
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 1 GO processes, IEA only
GO:0002250 adaptive immune response IBA
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 1 GO processes, IEA only
GO:0002250 adaptive immune response IBA

References

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1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. Berg LJ, Finkelstein LD, Lucas JA, Schwartzberg PL. (2005) Tec family kinases in T lymphocyte development and function. Annu. Rev. Immunol., 23: 549-600. [PMID:15771581]

3. Bradshaw JM, McFarland JM, Paavilainen VO, Bisconte A, Tam D, Phan VT, Romanov S, Finkle D, Shu J, Patel V et al.. (2015) Prolonged and tunable residence time using reversible covalent kinase inhibitors. Nat. Chem. Biol., 11 (7): 525-31. [PMID:26006010]

4. Byrd JC, Harrington B, O'Brien S, Jones JA, Schuh A, Devereux S, Chaves J, Wierda WG, Awan FT, Brown JR et al.. (2016) Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia. N. Engl. J. Med., 374 (4): 323-32. [PMID:26641137]

5. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

6. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

7. Li X, Zuo Y, Tang G, Wang Y, Zhou Y, Wang X, Guo T, Xia M, Ding N, Pan Z. (2014) Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity. J. Med. Chem., 57 (12): 5112-28. [PMID:24915291]

8. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

9. Zhong Y, Dong S, Strattan E, Ren L, Butchar JP, Thornton K, Mishra A, Porcu P, Bradshaw JM, Bisconte A et al.. (2015) Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694. J. Biol. Chem., 290 (10): 5960-78. [PMID:25593320]

How to cite this page

Tec family: tec protein tyrosine kinase. Last modified on 16/01/2018. Accessed on 22/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2238.