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Target not currently curated in GtoImmuPdb
Target id: 2105
Nomenclature: MAPK interacting serine/threonine kinase 2
Abbreviated Name: Mnk2
Family: MKN subfamily
Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 465 | 19p13.3 | MKNK2 | MAPK interacting serine/threonine kinase 2 | |
Mouse | - | 459 | 10 C1 | Mknk2 | MAP kinase-interacting serine/threonine kinase 2 | |
Rat | - | 459 | 7q11 | Mknk2 | MAPK interacting serine/threonine kinase 2 |
Database Links | |
Alphafold | Q9HBH9 (Hs), Q8CDB0 (Mm), Q5U2N4 (Rn) |
BRENDA | 2.7.11.1 |
ChEMBL Target | CHEMBL4204 (Hs), CHEMBL4523384 (Mm) |
Ensembl Gene | ENSG00000099875 (Hs), ENSMUSG00000020190 (Mm), ENSRNOG00000029028 (Rn) |
Entrez Gene | 2872 (Hs), 17347 (Mm), 299618 (Rn) |
Human Protein Atlas | ENSG00000099875 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:2872 (Hs), mmu:17347 (Mm), rno:299618 (Rn) |
OMIM | 605069 (Hs) |
Pharos | Q9HBH9 (Hs) |
RefSeq Nucleotide | NM_017572 (Hs), NM_021462 (Mm), NM_001011985 (Rn) |
RefSeq Protein | NP_060042 (Hs), NP_067437 (Mm), NP_001011985 (Rn) |
SynPHARM | 85807 (in complex with tomivosertib) |
UniProtKB | Q9HBH9 (Hs), Q8CDB0 (Mm), Q5U2N4 (Rn) |
Wikipedia | MKNK2 (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: 2,8 |
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Target used in screen: MKNK2 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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: 1,3 |
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Target used in screen: Mnk2/MNK2 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
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. 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]
3. 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]
4. Jauch R, Jäkel S, Netter C, Schreiter K, Aicher B, Jäckle H, Wahl MC. (2005) Crystal structures of the Mnk2 kinase domain reveal an inhibitory conformation and a zinc binding site. Structure, 13 (10): 1559-68. [PMID:16216586]
5. Johnson CN, Berdini V, Beke L, Bonnet P, Brehmer D, Coyle JE, Day PJ, Frederickson M, Freyne EJ, Gilissen RA et al.. (2014) Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase. ACS Med Chem Lett, 6 (1): 25-30. [PMID:25589925]
6. Oyarzabal J, Zarich N, Albarran MI, Palacios I, Urbano-Cuadrado M, Mateos G, Reymundo I, Rabal O, Salgado A, Corrionero A et al.. (2010) Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach. J Med Chem, 53 (18): 6618-28. [PMID:20722422]
7. Reich SH, Sprengeler PA, Chiang GG, Appleman JR, Chen J, Clarine J, Eam B, Ernst JT, Han Q, Goel VK et al.. (2018) Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition. J Med Chem, 61 (8): 3516-3540. [PMID:29526098]
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. Yang H, Chennamaneni LR, Ho MWT, Ang SH, Tan ESW, Jeyaraj DA, Yeap YS, Liu B, Ong EH, Joy JK et al.. (2018) Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia. J Med Chem, 61 (10): 4348-4369. [PMID:29683667]
10. Yuan X, Guan D, Chen C, Guo S, Wu H, Bu H, Yang CY, Wang M, Zhou J, Zhang H. (2024) Development of an Imidazopyridazine-Based MNK1/2 Inhibitor for the Treatment of Lymphoma. J Med Chem, 67 (7): 5437-5457. [PMID:38564512]
MKN subfamily: MAPK interacting serine/threonine kinase 2. Last modified on 04/04/2024. Accessed on 04/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2105.