General Information of Target

Target ID LDTP12523
Target Name Serine/threonine-protein kinase LATS2 (LATS2)
Gene Name LATS2
Gene ID 26524
Synonyms
KPM; Serine/threonine-protein kinase LATS2; EC 2.7.11.1; Kinase phosphorylated during mitosis protein; Large tumor suppressor homolog 2; Serine/threonine-protein kinase kpm; Warts-like kinase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSLVLLSLAALCRSAVPREPTVQCGSETGPSPEWMLQHDLIPGDLRDLRVEPVTTSVATG
DYSILMNVSWVLRADASIRLLKATKICVTGKSNFQSYSCVRCNYTEAFQTQTRPSGGKWT
FSYIGFPVELNTVYFIGAHNIPNANMNEDGPSMSVNFTSPGCLDHIMKYKKKCVKAGSLW
DPNITACKKNEETVEVNFTTTPLGNRYMALIQHSTIIGFSQVFEPHQKKQTRASVVIPVT
GDSEGATVQLTPYFPTCGSDCIRHKGTVVLCPQTGVPFPLDNNKSKPGGWLPLLLLSLLV
ATWVLVAGIYLMWRHERIKKTSFSTTTLLPPIKVLVVYPSEICFHHTICYFTEFLQNHCR
SEVILEKWQKKKIAEMGPVQWLATQKKAADKVVFLLSNDVNSVCDGTCGKSEGSPSENSQ
DLFPLAFNLFCSDLRSQIHLHKYVVVYFREIDTKDDYNALSVCPKYHLMKDATAFCAELL
HVKQQVSAGKRSQACHDGCCSL
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, AGC Ser/Thr protein kinase family
Subcellular location
Cytoplasm, cytoskeleton, microtubule organizing center, centrosome
Function
Negative regulator of YAP1 in the Hippo signaling pathway that plays a pivotal role in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein STK3/MST2 and STK4/MST1, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Phosphorylation of YAP1 by LATS2 inhibits its translocation into the nucleus to regulate cellular genes important for cell proliferation, cell death, and cell migration. Acts as a tumor suppressor which plays a critical role in centrosome duplication, maintenance of mitotic fidelity and genomic stability. Negatively regulates G1/S transition by down-regulating cyclin E/CDK2 kinase activity. Negative regulator of the androgen receptor. Phosphorylates SNAI1 in the nucleus leading to its nuclear retention and stabilization, which enhances its epithelial-mesenchymal transition and tumor cell invasion/migration activities. This tumor-promoting activity is independent of its effects upon YAP1 or WWTR1/TAZ.
TTD ID
T18390
Uniprot ID
Q9NRM7
DrugMap ID
TTML7FG
Ensemble ID
ENST00000382592.5
HGNC ID
HGNC:6515
ChEMBL ID
CHEMBL5907

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C905(1.96)  LDD3368  [1]
IA-alkyne
 Probe Info 
C112(9.98)  LDD0371  [2]
AMP probe
 Probe Info 
N.A.  LDD0200  [3]
ATP probe
 Probe Info 
N.A.  LDD0199  [3]
NAIA_5
 Probe Info 
C850(0.00); C813(0.00)  LDD2225  [4]
IPM
 Probe Info 
C637(0.00); C813(0.00)  LDD2156  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA HEK-293T C112(9.98)  LDD0371  [2]
 LDCM0026  4SU-RNA+native RNA HEK-293T C112(7.60)  LDD0372  [2]
 LDCM0632  CL-Sc Hep-G2 C813(0.33)  LDD2227  [4]
 LDCM0022  KB02 A204 C905(2.28)  LDD2252  [1]
 LDCM0023  KB03 A204 C905(2.19)  LDD2669  [1]
 LDCM0024  KB05 OAW-28 C905(1.96)  LDD3368  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
E3 ubiquitin-protein ligase SIAH2 (SIAH2) SINA (Seven in absentia) family O43255
DDB1- and CUL4-associated factor 1 (DCAF1) VPRBP/DCAF1 family Q9Y4B6
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
MOB kinase activator 1A (MOB1A) MOB1/phocein family Q9H8S9
MOB kinase activator 1B (MOB1B) MOB1/phocein family Q7L9L4
LIM domain-containing protein ajuba (AJUBA) Zyxin/ajuba family Q96IF1
Four and a half LIM domains protein 3 (FHL3) . Q13643

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid20684608c35 Small molecular drug D0R3MO

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
3 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
4 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
5 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019