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large tumor suppressor kinase 2

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Immunopharmacology Ligand target has curated data in GtoImmuPdb

Target id: 1516

Nomenclature: large tumor suppressor kinase 2

Abbreviated Name: LATS2

Family: NDR family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1088 13q12.11 LATS2 large tumor suppressor kinase 2
Mouse - 1042 14 C3 Lats2 large tumor suppressor 2
Rat - 1042 15p12 Lats2 large tumor suppressor kinase 2
Previous and Unofficial Names Click here for help
KPM | Large tumor suppressor homologue 2 | large tumor suppressor 2
Database Links Click here for help
BRENDA
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Solution structure of RSGI RUH-038, a UBA domain from Mouse LATS2 (Large Tumor Suppressor homolog 2)
PDB Id:  2COS
Resolution:  0.0Å
Species:  Mouse
References: 
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 35 [PMID: 20684608] Small molecule or natural product Click here for species-specific activity table Hs Inhibition - - 2
[2]
Description: Measured as % inhibition using 3μM compound.
Inhibitor Comments
3μM compound 35 [PMID 20684608] inhibits LATS2 activity by 75% [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: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: LATS2
Ligand Sp. Type Action Value Parameter
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 9.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
GSK690693 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
A-674563 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
ruboxistaurin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.2 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 5.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
LATS1 and LATS2 are included in the GToImmuPdb because of their crucial role in Hippo signalling, a major mammalian signalling cascade that has recently been identified as playing an important role in shaping the innate immune response [1-2,4].

References

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1. 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]

2. Fang X, Yin Y, Chen YT, Yao L, Wang B, Cameron MD, Lin L, Khan S, Ruiz C, Schröter T et al.. (2010) Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors. J. Med. Chem., 53 (15): 5727-37. [PMID:20684608]

3. 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

NDR family: large tumor suppressor kinase 2. Last modified on 04/06/2018. Accessed on 01/12/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1516.