Details of the Target

General Information of Target

Target ID LDTP00864
Target Name Alpha-endosulfine (ENSA)
Gene Name ENSA
Gene ID 2029
Synonyms
Alpha-endosulfine; ARPP-19e
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSQKQEEENPAEETGEEKQDTQEKEGILPERAEEAKLKAKYPSLGQKPGGSDFLMKRLQK
GQKYFDSGDYNMAKAKMKNKQLPSAGPDKNLVTGDHIPTPQDLPQRKSSLVTSKLAGGQV
E
Target Type
Literature-reported
Target Bioclass
Other
Family
Endosulfine family
Subcellular location
Cytoplasm
Function
Protein phosphatase inhibitor that specifically inhibits protein phosphatase 2A (PP2A) during mitosis. When phosphorylated at Ser-67 during mitosis, specifically interacts with PPP2R2D (PR55-delta) and inhibits its activity, leading to inactivation of PP2A, an essential condition to keep cyclin-B1-CDK1 activity high during M phase. Also acts as a stimulator of insulin secretion by interacting with sulfonylurea receptor (ABCC8), thereby preventing sulfonylurea from binding to its receptor and reducing K(ATP) channel currents.
TTD ID
T58460
Uniprot ID
O43768
DrugMap ID
TTQD0YT
Ensemble ID
ENST00000271690.12
HGNC ID
HGNC:3360

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AN3CA SNV: p.E16D .
GAMG SNV: p.G68A .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C-Sul
 Probe Info  		74.79  LDD0066  [1]
STPyne
 Probe Info  		K47(5.03); K56(2.65); K80(4.23)  LDD0277  [2]
ONAyne
 Probe Info  		N.A.  LDD0273  [2]
Probe 1
 Probe Info  		Y64(15.70); Y70(212.85)  LDD3495  [3]
5E-2FA
 Probe Info  		N.A.  LDD2235  [4]
ATP probe
 Probe Info  		K114(0.00); K80(0.00); K107(0.00); K56(0.00)  LDD0199  [5]
m-APA
 Probe Info  		N.A.  LDD2231  [4]
NHS
 Probe Info  		K63(0.00); K74(0.00); K47(0.00)  LDD0010  [6]
SF
 Probe Info  		Y64(0.00); Y70(0.00)  LDD0028  [7]
AOyne
 Probe Info  		13.50  LDD0443  [8]
HHS-465
 Probe Info  		K74(0.00); Y41(0.00); Y64(0.00); Y70(0.00)  LDD2240  [9]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C313
 Probe Info  		13.09  LDD1980  [10]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Fibroblast growth factor receptor 3 (FGFR3) Tyr protein kinase family P22607
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Adrenocortical dysplasia protein homolog (ACD) . Q96AP0
Ubiquilin-1 (UBQLN1) . Q9UMX0

References

1 Low-Toxicity Sulfonium-Based Probes for Cysteine-Specific Profiling in Live Cells. Anal Chem. 2022 Mar 15;94(10):4366-4372. doi: 10.1021/acs.analchem.1c05129. Epub 2022 Mar 4.
2 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
3 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
4 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
5 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.
6 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
7 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
8 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
9 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010
10 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587