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DM1 protein kinase

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Target not currently curated in GtoImmuPdb

Target id: 1505

Nomenclature: DM1 protein kinase

Abbreviated Name: DMPK1

Family: GEK subfamily

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 624 19q13.3 DMPK DM1 protein kinase
Mouse 1 631 7 Dmpk dystrophia myotonica-protein kinase
Rat - - 1q21 Dmpk DM1 protein kinase
Previous and Unofficial Names Click here for help
DM1 | Dm15 | DM1PK | DM protein kinase | dystrophia myotonica 1 | dystrophia myotonica kinase, B15 | dystrophia myotonica protein kinase | MDPK | MT-PK | myotonin protein kinase A
Database Links Click here for help
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  STRUCTURE OF HUMAN MYOTONIC DYSTROPHY PROTEIN KINASE IN COMPLEX WITH THE BISINDOYLMALEIDE INHIBITOR BIM VIII
PDB Id:  2VD5
Resolution:  2.8Å
Species:  Human
References:  3
Image of receptor 3D structure from RCSB PDB
Description:  Coiled-Coil domain of DMPK
PDB Id:  1WT6
Resolution:  1.6Å
Species:  Human
References:  5
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
RKI-1447 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 6
pIC50 7.5 (IC50 3.406x10-8 M) [6]
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: 2,7

Key to terms and symbols Click column headers to sort
Target used in screen: DMPK
Ligand Sp. Type Action Value Parameter
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.0 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
PP-242 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
R547 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
alvocidib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 pKd
AT-7519 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.0 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: DMPK/DMPK
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 4.8 13.5 7.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 78.4 122.0 31.0
p38 MAP kinase inhibitor III Small molecule or natural product Hs Inhibitor Inhibition 80.0 115.0 105.0
aloisine Small molecule or natural product Hs Inhibitor Inhibition 84.3 95.0 101.0
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 84.8 127.0 148.0
ATM/ATR kinase inhibitor Small molecule or natural product Hs Inhibitor Inhibition 85.5 71.0 106.0
p38 MAP kinase inhibitor Small molecule or natural product Hs Inhibitor Inhibition 87.6 113.0 99.0
BAY 11-7082 Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 89.0 125.0 100.0
alsterpaullone 2-cyanoethyl Small molecule or natural product Hs Inhibitor Inhibition 89.8 109.0 76.0
gefitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 90.1
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Myotonic dystrophy 1
Synonyms: Steinert myotonic dystrophy [Orphanet: ORPHA273]
Disease Ontology: DOID:11722
OMIM: 160900
Orphanet: ORPHA273

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. Elkins JM, Amos A, Niesen FH, Pike AC, Fedorov O, Knapp S. (2009) Structure of dystrophia myotonica protein kinase. Protein Sci., 18 (4): 782-91. [PMID:19309729]

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. Garcia P, Ucurum Z, Bucher R, Svergun DI, Huber T, Lustig A, Konarev PV, Marino M, Mayans O. (2006) Molecular insights into the self-assembly mechanism of dystrophia myotonica kinase. FASEB J., 20 (8): 1142-51. [PMID:16770013]

6. Pireddu R, Forinash KD, Sun NN, Martin MP, Sung SS, Alexander B, Zhu JY, Guida WC, Schönbrunn E, Sebti SM et al.. (2012) Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2). Medchemcomm, 3 (6): 699-709. [PMID:23275831]

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

GEK subfamily: DM1 protein kinase. Last modified on 18/08/2017. Accessed on 26/10/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1505.