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Gene and Protein Information | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | - | 1332 | 17p13.2 | MINK1 | misshapen like kinase 1 | |
Mouse | - | 1308 | 11 B3 | Mink1 | misshapen-like kinase 1 (zebrafish) | |
Rat | - | 1336 | 10q24 | Mink1 | misshapen-like kinase 1 |
Previous and Unofficial Names |
GCK family kinase MiNK | MAP4K6 | MAPK/ERK kinase kinase kinase 6 | MEK kinase kinase 6 | MEKKK 6 | MINK | YSK2 | ZC3 |
Database Links | |
Alphafold | Q8N4C8 (Hs), Q9JM52 (Mm), F1LP90 (Rn) |
BRENDA | 2.7.11.1 |
CATH/Gene3D | 1.25.10.10 |
ChEMBL Target | CHEMBL5518 (Hs) |
Ensembl Gene | ENSG00000141503 (Hs), ENSMUSG00000020827 (Mm), ENSRNOG00000033508 (Rn) |
Entrez Gene | 50488 (Hs), 50932 (Mm), 303259 (Rn) |
Human Protein Atlas | ENSG00000141503 (Hs) |
KEGG Enzyme | 2.7.11.1 |
KEGG Gene | hsa:50488 (Hs), mmu:50932 (Mm), rno:303259 (Rn) |
OMIM | 609426 (Hs) |
Pharos | Q8N4C8 (Hs) |
RefSeq Nucleotide | NM_001024937 (Hs), NM_001045959 (Mm), NM_001271136 (Rn) |
RefSeq Protein | NP_001020108 (Hs), NP_001039424 (Mm), NP_001258065 (Rn) |
UniProtKB | Q8N4C8 (Hs), Q9JM52 (Mm), F1LP90 (Rn) |
Wikipedia | MINK1 (Hs) |
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: 5,11 |
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Target used in screen: MINK | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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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: 2,6 |
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Target used in screen: MINK/MINK(MINK1) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Displaying the top 10 most potent ligands View all ligands in screen » |
Immunopharmacology Comments |
MINK promotes the negative selection of autoreactive thymocytes during T cell development, an action that is effected by JNK-mediated apoptosis [9]. |
Immuno Process Associations | ||
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General Comments |
MINK (MINK1, also known as MAP4K6) is ubiquitously expressed in mice and humans, and is found in most tissues [4,7]. Exogenously expressed MINK activates the JNK pathway and p38 signalling in vitro, and studies in cell lines indicate roles for MINK in the regulation of cytoskeletal reorganisation, cell adhesion, and cell motility (NCK(TNIK)-dependent activities), and neuronal structure and function (via activation of Rap2 (RAP2A), a Ras family GTPase) [8]. |
1. Ammirati M, Bagley SW, Bhattacharya SK, Buckbinder L, Carlo AA, Conrad R, Cortes C, Dow RL, Dowling MS, El-Kattan A et al.. (2015) Discovery of an in Vivo Tool to Establish Proof-of-Concept for MAP4K4-Based Antidiabetic Treatment. ACS Med Chem Lett, 6 (11): 1128-33. [PMID:26617966]
2. 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]
3. 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]
4. Dan I, Watanabe NM, Kobayashi T, Yamashita-Suzuki K, Fukagaya Y, Kajikawa E, Kimura WK, Nakashima TM, Matsumoto K, Ninomiya-Tsuji J et al.. (2000) Molecular cloning of MINK, a novel member of mammalian GCK family kinases, which is up-regulated during postnatal mouse cerebral development. FEBS Lett, 469 (1): 19-23. [PMID:10708748]
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. Hu Y, Leo C, Yu S, Huang BC, Wang H, Shen M, Luo Y, Daniel-Issakani S, Payan DG, Xu X. (2004) Identification and functional characterization of a novel human misshapen/Nck interacting kinase-related kinase, hMINK beta. J Biol Chem, 279 (52): 54387-97. [PMID:15469942]
8. Hussain NK, Hsin H, Huganir RL, Sheng M. (2010) MINK and TNIK differentially act on Rap2-mediated signal transduction to regulate neuronal structure and AMPA receptor function. J Neurosci, 30 (44): 14786-94. [PMID:21048137]
9. McCarty N, Paust S, Ikizawa K, Dan I, Li X, Cantor H. (2005) Signaling by the kinase MINK is essential in the negative selection of autoreactive thymocytes. Nat Immunol, 6 (1): 65-72. [PMID:15608642]
10. Millan DS, Bunnage ME, Burrows JL, Butcher KJ, Dodd PG, Evans TJ, Fairman DA, Hughes SJ, Kilty IC, Lemaitre A et al.. (2011) Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease. J Med Chem, 54 (22): 7797-814. [PMID:21888439]
11. 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]
MSN subfamily: misshapen like kinase 1. Last modified on 19/03/2024. Accessed on 02/11/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2103.