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MAPK activated protein kinase 3

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Target id: 2095

Nomenclature: MAPK activated protein kinase 3

Abbreviated Name: MAPKAPK3

Family: MAPKAPK subfamily

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 382 3p21.2 MAPKAPK3 MAPK activated protein kinase 3
Mouse - 384 9 F1 Mapkapk3 mitogen-activated protein kinase-activated protein kinase 3
Rat - 384 8q32 Mapkapk3 MAPK activated protein kinase 3
Previous and Unofficial Names Click here for help
MAPKAP kinase 3 | mitogen-activated protein kinase-activated protein kinase 3
Database Links Click here for help
Alphafold Q16644 (Hs), Q3UMW7 (Mm), Q66H84 (Rn)
BRENDA 2.7.11.1
CATH/Gene3D 4.10.1170.10
ChEMBL Target CHEMBL4670 (Hs)
Ensembl Gene ENSG00000114738 (Hs), ENSMUSG00000032577 (Mm), ENSRNOG00000014832 (Rn)
Entrez Gene 7867 (Hs), 102626 (Mm), 315994 (Rn)
Human Protein Atlas ENSG00000114738 (Hs)
KEGG Enzyme 2.7.11.1
KEGG Gene hsa:7867 (Hs), mmu:102626 (Mm), rno:315994 (Rn)
OMIM 602130 (Hs)
Pharos Q16644 (Hs)
RefSeq Nucleotide NM_001243925 (Hs), NM_178907 (Mm), NM_001012127 (Rn)
RefSeq Protein NP_004626 (Hs), NP_849238 (Mm), NP_001012127 (Rn)
UniProtKB Q16644 (Hs), Q3UMW7 (Mm), Q66H84 (Rn)
Wikipedia MAPKAPK3 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  High resolution crystal structure of mitogen-activated protein kinase-activated protein kinase 3 (MK3)-inhibitor complex
PDB Id:  3FHR
Resolution:  1.9Å
Species:  Human
References:  3
Enzyme Reaction Click here for help
EC Number: 2.7.11.1

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
compound 16 [PMID: 17480064] Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.7 pIC50 2
⤷ pIC50 6.7 (IC50 2.1x10-7 M) [2]
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: MAPKAP-K3/MAPKAPK3
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Small molecule or natural product Hs Inhibitor Inhibition 54.7 47.0 2.0
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 76.0 105.0 108.0
Cdk4 inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 76.5 85.0 61.0
GSK-3 inhibitor XIII Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 81.0 100.0 91.0
chelerythrine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 83.0 99.0 53.0
Gö 6976 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 83.7 131.0 77.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 85.1 97.0 44.5
Chk2 inhibitor II Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 85.3 111.0 127.0
purvalanol A Small molecule or natural product Hs Inhibitor Inhibition 85.4 124.0 84.0
casein kinase II inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 86.3 107.0 82.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Antigen presentation
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Cellular signalling

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. Anderson DR, Meyers MJ, Vernier WF, Mahoney MW, Kurumbail RG, Caspers N, Poda GI, Schindler JF, Reitz DB, Mourey RJ. (2007) Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J Med Chem, 50 (11): 2647-54. [PMID:17480064]

3. Cheng R, Felicetti B, Palan S, Toogood-Johnson I, Scheich C, Barker J, Whittaker M, Hesterkamp T. (2010) High-resolution crystal structure of human Mapkap kinase 3 in complex with a high affinity ligand. Protein Sci, 19 (1): 168-73. [PMID:19937655]

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]

How to cite this page

MAPKAPK subfamily: MAPK activated protein kinase 3. Last modified on 30/04/2019. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2095.