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microtubule affinity regulating kinase 2

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Target id: 2098

Nomenclature: microtubule affinity regulating kinase 2

Abbreviated Name: MARK2

Family: MARK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 788 11q13.1 MARK2 microtubule affinity regulating kinase 2
Mouse - 776 19 5.32 cM Mark2 MAP/microtubule affinity regulating kinase 2
Rat - 722 1q43 Mark2 microtubule affinity regulating kinase 2
Previous and Unofficial Names Click here for help
EMK1 | ELKL motif kinase 1 | Par-1 | MAP/microtubule affinity-regulating kinase 2
Database Links Click here for help
Alphafold Q7KZI7 (Hs), Q05512 (Mm), O08679 (Rn)
BRENDA 2.7.11.1, 2.7.11.26
ChEMBL Target CHEMBL3831 (Hs)
Ensembl Gene ENSG00000072518 (Hs), ENSMUSG00000024969 (Mm), ENSRNOG00000021184 (Rn)
Entrez Gene 2011 (Hs), 13728 (Mm), 60328 (Rn)
Human Protein Atlas ENSG00000072518 (Hs)
KEGG Enzyme 2.7.11.1, 2.7.11.26
KEGG Gene hsa:2011 (Hs), mmu:13728 (Mm), rno:60328 (Rn)
OMIM 600526 (Hs)
Pharos Q7KZI7 (Hs)
RefSeq Nucleotide NM_001039469 (Hs), NM_004954 (Mm), NM_021699 (Rn)
RefSeq Protein NP_004945 (Hs), NP_001073857 (Mm), NP_067731 (Rn)
UniProtKB Q7KZI7 (Hs), Q05512 (Mm), O08679 (Rn)
Wikipedia MARK2 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Helicobacter pylori CagA Inhibits PAR1/MARK Family Kinases by Mimicking Host Substrates
PDB Id:  3IEC
Resolution:  2.2Å
Species:  Human
References:  4
Enzyme Reaction Click here for help
EC Number: 2.7.11.1
EC Number: 2.7.11.26

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
PCC0105003 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.7 pIC50 5
⤷ pIC50 8.7 (IC50 2x10-9 M) [5]
DiscoveRx KINOMEscan® screen Click here for help
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: 2,6
Key to terms and symbols Click column headers to sort
Target used in screen: MARK2
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.1 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.0 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.5 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
ruxolitinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.2 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.1 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
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
Key to terms and symbols Click column headers to sort
Target used in screen: PAR-1Bα/MARK2(PAR-1Ba)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 0.0 -1.0 0.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 1.6 1.0 -2.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 3.3 1.0 2.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 3.4 4.0 -1.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 3.5 0.0 2.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 4.9 63.0 36.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.7 11.0 3.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 11.8 5.0 9.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 16.7 10.0 4.0
isogranulatimide Small molecule or natural product Hs Inhibitor Inhibition 34.7 40.0 20.0
Displaying the top 10 most potent ligands  View all ligands in screen »

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. 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. Nesić D, Miller MC, Quinkert ZT, Stein M, Chait BT, Stebbins CE. (2010) Helicobacter pylori CagA inhibits PAR1-MARK family kinases by mimicking host substrates. Nat Struct Mol Biol, 17 (1): 130-2. [PMID:19966800]

5. Shi YQ, Sun ZH, Wang ZZ, Su CY, Zhang W, Yu LY, Xu Y, Gao YL, Wang HB, Tian JW et al.. (2023) A novel role for microtubule affinity-regulating kinases in neuropathic pain. Br J Pharmacol, [Epub ahead of print]. [PMID:38112022]

6. 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]

How to cite this page

MARK subfamily: microtubule affinity regulating kinase 2. Last modified on 12/03/2024. Accessed on 17/09/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2098.