General Information of Target

Target ID LDTP03811
Target Name V-type proton ATPase subunit E 1 (ATP6V1E1)
Gene Name ATP6V1E1
Gene ID 529
Synonyms
ATP6E; ATP6E2; V-type proton ATPase subunit E 1; V-ATPase subunit E 1; V-ATPase 31 kDa subunit; p31; Vacuolar proton pump subunit E 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MALSDADVQKQIKHMMAFIEQEANEKAEEIDAKAEEEFNIEKGRLVQTQRLKIMEYYEKK
EKQIEQQKKIQMSNLMNQARLKVLRARDDLITDLLNEAKQRLSKVVKDTTRYQVLLDGLV
LQGLYQLLEPRMIVRCRKQDFPLVKAAVQKAIPMYKIATKNDVDVQIDQESYLPEDIAGG
VEIYNGDRKIKVSNTLESRLDLIAQQMMPEVRGALFGANANRKFLD
Target Bioclass
Transporter and channel
Family
V-ATPase E subunit family
Subcellular location
Apical cell membrane
Function
Subunit of the V1 complex of vacuolar(H+)-ATPase (V-ATPase), a multisubunit enzyme composed of a peripheral complex (V1) that hydrolyzes ATP and a membrane integral complex (V0) that translocates protons. V-ATPase is responsible for acidifying and maintaining the pH of intracellular compartments and in some cell types, is targeted to the plasma membrane, where it is responsible for acidifying the extracellular environment.
Uniprot ID
P36543
Ensemble ID
ENST00000253413.10
HGNC ID
HGNC:857

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
MCAS SNV: p.D201N .
TOV21G SNV: p.S193Y .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 13 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info 
K107(4.00); K138(10.00); K145(0.17); K156(10.00)  LDD0277  [1]
Probe 1
 Probe Info 
Y56(43.43); Y57(34.57)  LDD3495  [2]
m-APA
 Probe Info 
9.48  LDD0403  [3]
HHS-482
 Probe Info 
Y56(0.77)  LDD0285  [4]
HHS-475
 Probe Info 
Y184(0.36); Y56(0.85)  LDD0264  [5]
HHS-465
 Probe Info 
Y56(10.00)  LDD2237  [6]
5E-2FA
 Probe Info 
N.A.  LDD2235  [7]
ATP probe
 Probe Info 
N.A.  LDD0199  [8]
SF
 Probe Info 
Y57(0.00); Y56(0.00)  LDD0028  [9]
1c-yne
 Probe Info 
K191(0.00); K10(0.00)  LDD0228  [10]
MPP-AC
 Probe Info 
N.A.  LDD0428  [11]
TER-AC
 Probe Info 
N.A.  LDD0426  [11]
TPP-AC
 Probe Info 
N.A.  LDD0427  [11]
PAL-AfBPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C040
 Probe Info 
9.51  LDD1740  [12]
C210
 Probe Info 
62.68  LDD1884  [12]
C244
 Probe Info 
17.75  LDD1917  [12]
C310
 Probe Info 
7.89  LDD1977  [12]
FFF probe13
 Probe Info 
6.54  LDD0476  [13]
FFF probe3
 Probe Info 
17.15  LDD0464  [13]
VE-P
 Probe Info 
N.A.  LDD0396  [14]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0156  Aniline NCI-H1299 9.48  LDD0403  [3]
 LDCM0116  HHS-0101 DM93 Y184(0.36); Y56(0.85)  LDD0264  [5]
 LDCM0117  HHS-0201 DM93 Y184(0.63); Y56(0.76)  LDD0265  [5]
 LDCM0118  HHS-0301 DM93 Y184(0.61); Y56(0.87)  LDD0266  [5]
 LDCM0119  HHS-0401 DM93 Y184(0.63); Y56(0.79)  LDD0267  [5]
 LDCM0120  HHS-0701 DM93 Y184(0.73); Y56(0.93)  LDD0268  [5]
 LDCM0123  JWB131 DM93 Y56(0.77)  LDD0285  [4]
 LDCM0124  JWB142 DM93 Y56(0.87)  LDD0286  [4]
 LDCM0125  JWB146 DM93 Y56(0.81)  LDD0287  [4]
 LDCM0126  JWB150 DM93 Y56(2.22)  LDD0288  [4]
 LDCM0127  JWB152 DM93 Y56(1.77)  LDD0289  [4]
 LDCM0128  JWB198 DM93 Y56(1.18)  LDD0290  [4]
 LDCM0129  JWB202 DM93 Y56(0.76)  LDD0291  [4]
 LDCM0130  JWB211 DM93 Y56(1.02)  LDD0292  [4]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tiludronic Acid Small molecular drug DB01133

References

1 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
2 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.
3 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
4 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
5 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
6 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
7 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
8 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.
9 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
10 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
11 Differently Tagged Probes for Protein Profiling of Mitochondria. Chembiochem. 2019 May 2;20(9):1155-1160. doi: 10.1002/cbic.201800735. Epub 2019 Mar 26.
12 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
13 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
14 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.