mitogen-activated protein kinase kinase kinase 19 | STE20 family | IUPHAR Guide to IMMUNOPHARMACOLOGY

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mitogen-activated protein kinase kinase kinase 19

Target id: 2076

Nomenclature: mitogen-activated protein kinase kinase kinase 19

Abbreviated Name: YSK4

Family: STE20 family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: ON :     mitogen-activated protein kinase kinase kinase 19 has curated data in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1328 2q21.3 MAP3K19 mitogen-activated protein kinase kinase kinase 19
Mouse - 1311 1 E3 Map3k19 mitogen-activated protein kinase kinase kinase 19
Rat - 1306 13q12 Map3k19 mitogen-activated protein kinase kinase kinase 19
Previous and Unofficial Names
RCK | Regulated in COPD, protein kinase | Sps1/Ste20-related protein kinase YSK4
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.1

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
Ligand Sp. Action Affinity Units Reference
compound 1 [PMID: 24793884] Hs Inhibition - - 4
[4]
Description: Measured as % inhibition using 1μM compound.
Inhibitor Comments
MAP3K19 activity is inhibited by approximately 96% in the presence of 1μM compound 1 [PMID 24793884] [4] (note that MAP3K19 is referred to by its synonym YSK4 in the article's Supplementary data table)..
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: 3,5

Key to terms and symbols Click column headers to sort
Target used in screen: YSK4
Ligand Sp. Type Action Affinity Units
lestaurtinib Hs Inhibitor Inhibition 9.3 pKd
staurosporine Hs Inhibitor Inhibition 9.1 pKd
PP-242 Hs Inhibitor Inhibition 8.3 pKd
KW-2449 Hs Inhibitor Inhibition 8.3 pKd
foretinib Hs Inhibitor Inhibition 8.3 pKd
dovitinib Hs Inhibitor Inhibition 7.9 pKd
SU-14813 Hs Inhibitor Inhibition 7.9 pKd
midostaurin Hs Inhibitor Inhibition 7.8 pKd
neratinib Hs Inhibitor Inhibition 7.8 pKd
bosutinib Hs Inhibitor Inhibition 7.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. Boehme SA, Franz-Bacon K, DiTirro DN, Ly TW, Bacon KB. (2016) MAP3K19 Is a Novel Regulator of TGF-β Signaling That Impacts Bleomycin-Induced Lung Injury and Pulmonary Fibrosis. PLoS ONE, 11 (5): e0154874. [PMID:27144281]

2. Boehme SA, Franz-Bacon K, Ludka J, DiTirro DN, Ly TW, Bacon KB. (2016) MAP3K19 Is Overexpressed in COPD and Is a Central Mediator of Cigarette Smoke-Induced Pulmonary Inflammation and Lower Airway Destruction. PLoS ONE, 11 (12): e0167169. [PMID:27935962]

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. Reichelt A, Bailis JM, Bartberger MD, Yao G, Shu H, Kaller MR, Allen JG, Weidner MF, Keegan KS, Dao JH. (2014) Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. Eur J Med Chem, 80: 364-82. [PMID:24793884]

5. 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

STE20 family: mitogen-activated protein kinase kinase kinase 19. Last modified on 14/03/2017. Accessed on 19/01/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2076.