serine/threonine kinase 11

Target id: 2212

Nomenclature: serine/threonine kinase 11

Abbreviated Name: LKB1

Family: LKB subfamily

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 433 19p13.3 STK11 serine/threonine kinase 11
Mouse - 436 10 C1 Stk11 serine/threonine kinase 11
Rat - 436 7 q11 Stk11 serine/threonine kinase 11
Previous and Unofficial Names
liver kinase B1 homolog
Par-4
PJS
polarization-related protein LKB1
serine/threonine kinase 11 (Peutz-Jeghers syndrome)
Database Links
BRENDA
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG BRITE Hierarchy
KEGG Gene
OMIM
Orphanet Gene
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Structure of the heterotrimeric IKB1-STRADalpha-MO25alpha complex.
PDB Id:  2WTK
Resolution:  2.65Å
Species:  Human
References:  5
Enzyme Reaction
EC Number: 2.7.11.1
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: 2,4

Key to terms and symbols Click column headers to sort
Target used in screen: LKB1
Ligand Sp. Type Action Affinity Units
sunitinib Hs Inhibitor Inhibition 7.42 pKd
lestaurtinib Hs Inhibitor Inhibition 7.24 pKd
staurosporine Hs Inhibitor Inhibition 7.21 pKd
KW-2449 Hs Inhibitor Inhibition 6.62 pKd
fedratinib Hs Inhibitor Inhibition 6.51 pKd
midostaurin Hs Inhibitor Inhibition 6.46 pKd
SU-14813 Hs Inhibitor Inhibition 6.44 pKd
tozasertib Hs Inhibitor Inhibition 5.89 pKd
PHA-665752 Hs Inhibitor Inhibition 5.59 pKd
SB203580 Hs Inhibitor Inhibition <5.52 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
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: LKB1/LKB1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
indirubin derivative E804 Hs Inhibitor Inhibition 5.8 30.0 3.0
GSK-3beta inhibitor XII Hs Inhibitor Inhibition 12.4 67.0 11.0
PKR inhibitor Hs Inhibitor Inhibition 13.5 21.0 1.0
staurosporine Hs Inhibitor Inhibition 18.7 77.0 20.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 23.5 87.0 41.0
indirubin-3'-monoxime Hs Inhibitor Inhibition 25.6 83.0 44.0
Gö 6976 Hs Inhibitor Inhibition 31.8 82.0 96.0
aloisine A Hs Inhibitor Inhibition 33.5 97.0 73.0
JAK3 inhibitor VI Hs Inhibitor Inhibition 34.8 90.0 55.0
K-252a Hs Inhibitor Inhibition 41.4 97.0 74.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Peutz-Jeghers syndrome
OMIM:  175200
Orphanet:  2869
Disease:  Testicular germ cell tumor
OMIM:  273300

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. 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. 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]

5. Zeqiraj E, Filippi BM, Deak M, Alessi DR, van Aalten DM. (2009) Structure of the LKB1-STRAD-MO25 complex reveals an allosteric mechanism of kinase activation. Science326 (5960): 1707-11. [PMID:19892943]

How to cite this page

LKB subfamily: serine/threonine kinase 11. Last modified on 18/08/2014. Accessed on 27/11/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2212.