Top ▲

microtubule affinity regulating kinase 1

Click here for help

Target not currently curated in GtoImmuPdb

Target id: 2097

Nomenclature: microtubule affinity regulating kinase 1

Abbreviated Name: MARK1

Family: MARK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 795 1q41 MARK1 microtubule affinity regulating kinase 1
Mouse - 795 1 H5 Mark1 MAP/microtubule affinity regulating kinase 1
Rat - 793 13q26 Mark1 microtubule affinity regulating kinase 1
Previous and Unofficial Names Click here for help
Emk3 | Par1c | ELKL motif serine/threonine-protein kinase 3 | MAP/microtubule affinity-regulating kinase 1
Database Links Click here for help
Alphafold Q9P0L2 (Hs), Q8VHJ5 (Mm), O08678 (Rn)
BRENDA 2.7.11.1, 2.7.11.26
ChEMBL Target CHEMBL5940 (Hs)
Ensembl Gene ENSG00000116141 (Hs), ENSMUSG00000026620 (Mm), ENSRNOG00000002339 (Rn)
Entrez Gene 4139 (Hs), 226778 (Mm), 117016 (Rn)
Human Protein Atlas ENSG00000116141 (Hs)
KEGG Enzyme 2.7.11.1, 2.7.11.26
KEGG Gene hsa:4139 (Hs), mmu:226778 (Mm), rno:117016 (Rn)
OMIM 606511 (Hs)
Pharos Q9P0L2 (Hs)
RefSeq Nucleotide NM_018650 (Hs), NM_145515 (Mm), NM_053947 (Rn)
RefSeq Protein NP_061120 (Hs), NP_663490 (Mm), NP_446399 (Rn)
UniProtKB Q9P0L2 (Hs), Q8VHJ5 (Mm), O08678 (Rn)
Wikipedia MARK1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the Kinase Associated Domain 1 (KA1) from MARK1 kinase
PDB Id:  3OSE
Resolution:  1.7Å
Species:  Human
References:  5
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 8.5 pIC50 6
⤷ pIC50 8.5 (IC50 3x10-9 M) [6]
7-hydroxystaurosporine Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.6 pIC50 2
⤷ pIC50 7.6 (IC50 2.7x10-8 M) [2]
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: 3,7
Key to terms and symbols Click column headers to sort
Target used in screen: MARK1
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
lestaurtinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.8 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.5 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 5.9 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 5.6 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: 1,4
Key to terms and symbols Click column headers to sort
Target used in screen: MARK1/MARK1
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 0.2 -0.5 0.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 1.3 0.0 0.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 2.7 -1.0 0.0
JAK3 inhibitor VI Small molecule or natural product Hs Inhibitor Inhibition 3.3 1.0 0.0
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 4.1 1.0 0.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 10.4 38.0 29.0
SU11652 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 18.1 14.0 3.0
PKR inhibitor Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.0 9.0 0.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 20.8 4.0 5.0
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 34.8
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

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. Busby EC, Leistritz DF, Abraham RT, Karnitz LM, Sarkaria JN. (2000) The radiosensitizing agent 7-hydroxystaurosporine (UCN-01) inhibits the DNA damage checkpoint kinase hChk1. Cancer Res, 60 (8): 2108-12. [PMID:10786669]

3. 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]

4. 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]

5. Moravcevic K, Mendrola JM, Schmitz KR, Wang YH, Slochower D, Janmey PA, Lemmon MA. (2010) Kinase associated-1 domains drive MARK/PAR1 kinases to membrane targets by binding acidic phospholipids. Cell, 143 (6): 966-77. [PMID:21145462]

6. 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]

7. 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 1. Last modified on 12/03/2024. Accessed on 18/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2097.