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Target id: 2032
Nomenclature: HCK proto-oncogene, Src family tyrosine kinase
Abbreviated Name: Hck
Family: Src family
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 526 | 20q11.21 | HCK | HCK proto-oncogene, Src family tyrosine kinase | |
Mouse | - | 524 | 2 75.41 cM | Hck | hemopoietic cell kinase | |
Rat | - | 524 | 3q41 | Hck | HCK proto-oncogene, Src family tyrosine kinase |
Previous and Unofficial Names |
Bmk | JTK9 | p56Hck | hemopoietic cell kinase | HCK proto-oncogene |
Database Links | |
Alphafold | P08631 (Hs), P08103 (Mm), P50545 (Rn) |
BRENDA | 2.7.10.2 |
CATH/Gene3D | 3.30.505.10 |
ChEMBL Target | CHEMBL3234 (Hs) |
Ensembl Gene | ENSG00000101336 (Hs), ENSMUSG00000003283 (Mm), ENSRNOG00000009331 (Rn) |
Entrez Gene | 3055 (Hs), 15162 (Mm), 25734 (Rn) |
Human Protein Atlas | ENSG00000101336 (Hs) |
KEGG Enzyme | 2.7.10.2 |
KEGG Gene | hsa:3055 (Hs), mmu:15162 (Mm), rno:25734 (Rn) |
OMIM | 142370 (Hs) |
Pharos | P08631 (Hs) |
RefSeq Nucleotide | NM_001172129 (Hs), NM_010407 (Mm), NM_013185 (Rn) |
RefSeq Protein | NP_002101 (Hs), NP_034537 (Mm), NP_037317 (Rn) |
SynPHARM | 80998 (in complex with PP121) |
UniProtKB | P08631 (Hs), P08103 (Mm), P50545 (Rn) |
Wikipedia | HCK (Hs) |
Selected 3D Structures | |||||||||||
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Enzyme Reaction | ||||
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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 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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: 8,13 |
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Target used in screen: HCK | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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: 1,10 |
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Target used in screen: Hck (activated)/nd | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Target used in screen: Hck/HCK | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
Hck is thought to be involved in neutrophil migration, potentially via binding to intergrins [5]. |
Cell Type Associations | ||||||
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Immuno Process Associations | ||
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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. Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA. (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol, 4 (11): 691-9. [PMID:18849971]
3. Arold S, O'Brien R, Franken P, Strub MP, Hoh F, Dumas C, Ladbury JE. (1998) RT loop flexibility enhances the specificity of Src family SH3 domains for HIV-1 Nef. Biochemistry, 37 (42): 14683-91. [PMID:9778343]
4. Bachegowda L, Morrone K, Winski SL, Mantzaris I, Bartenstein M, Ramachandra N, Giricz O, Sukrithan V, Nwankwo G, Shahnaz S et al.. (2016) Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia. Cancer Res, 76 (16): 4841-4849. [PMID:27287719]
5. Baruzzi A, Iacobucci I, Soverini S, Lowell CA, Martinelli G, Berton G. (2010) c-Abl and Src-family kinases cross-talk in regulation of myeloid cell migration. FEBS Lett, 584 (1): 15-21. [PMID:19903482]
6. 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]
7. Chen P, Norris D, Das J, Spergel SH, Wityak J, Leith L, Zhao R, Chen BC, Pitt S, Pang S et al.. (2004) Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors. Bioorg Med Chem Lett, 14 (24): 6061-6. [PMID:15546730]
8. 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]
9. Fraser C, Dawson JC, Dowling R, Houston DR, Weiss JT, Munro AF, Muir M, Harrington L, Webster SP, Frame MC et al.. (2016) Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. J Med Chem, 59 (10): 4697-710. [PMID:27115835]
10. 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]
11. Lowell CA. (2004) Src-family kinases: rheostats of immune cell signaling. Mol Immunol, 41 (6-7): 631-43. [PMID:15220000]
12. Schindler T, Sicheri F, Pico A, Gazit A, Levitzki A, Kuriyan J. (1999) Crystal structure of Hck in complex with a Src family-selective tyrosine kinase inhibitor. Mol Cell, 3 (5): 639-48. [PMID:10360180]
13. 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]
Src family: HCK proto-oncogene, Src family tyrosine kinase. Last modified on 24/04/2018. Accessed on 10/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2032.