General Information of Target

Target ID LDTP06499
Target Name V-type proton ATPase subunit S1 (ATP6AP1)
Gene Name ATP6AP1
Gene ID 537
Synonyms
ATP6IP1; ATP6S1; VATPS1; XAP3; V-type proton ATPase subunit S1; V-ATPase subunit S1; Protein XAP-3; V-ATPase Ac45 subunit; V-ATPase S1 accessory protein; Vacuolar proton pump subunit S1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MMAAMATARVRMGPRCAQALWRMPWLPVFLSLAAAAAAAAAEQQVPLVLWSSDRDLWAPA
ADTHEGHITSDLQLSTYLDPALELGPRNVLLFLQDKLSIEDFTAYGGVFGNKQDSAFSNL
ENALDLAPSSLVLPAVDWYAVSTLTTYLQEKLGASPLHVDLATLRELKLNASLPALLLIR
LPYTASSGLMAPREVLTGNDEVIGQVLSTLKSEDVPYTAALTAVRPSRVARDVAVVAGGL
GRQLLQKQPVSPVIHPPVSYNDTAPRILFWAQNFSVAYKDQWEDLTPLTFGVQELNLTGS
FWNDSFARLSLTYERLFGTTVTFKFILANRLYPVSARHWFTMERLEVHSNGSVAYFNASQ
VTGPSIYSFHCEYVSSLSKKGSLLVARTQPSPWQMMLQDFQIQAFNVMGEQFSYASDCAS
FFSPGIWMGLLTSLFMLFIFTYGLHMILSLKTMDRFDDHKGPTISLTQIV
Target Bioclass
Transporter and channel
Family
Vacuolar ATPase subunit S1 family
Subcellular location
Endoplasmic reticulum membrane
Function
Accessory subunit of the proton-transporting vacuolar (V)-ATPase protein pump, which is required for luminal acidification of secretory vesicles. Guides the V-type ATPase into specialized subcellular compartments, such as neuroendocrine regulated secretory vesicles or the ruffled border of the osteoclast, thereby regulating its activity. Involved in membrane trafficking and Ca(2+)-dependent membrane fusion. May play a role in the assembly of the V-type ATPase complex (Probable). In aerobic conditions, involved in intracellular iron homeostasis, thus triggering the activity of Fe(2+) prolyl hydroxylase (PHD) enzymes, and leading to HIF1A hydroxylation and subsequent proteasomal degradation. In islets of Langerhans cells, may regulate the acidification of dense-core secretory granules.
TTD ID
T01211
Uniprot ID
Q15904
DrugMap ID
TTWDM4U
Ensemble ID
ENST00000369762.7
HGNC ID
HGNC:868
ChEMBL ID
CHEMBL4790

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FBPP2
 Probe Info 
5.17  LDD0318  [1]
OPA-S-S-alkyne
 Probe Info 
K380(1.79)  LDD3494  [2]
Probe 1
 Probe Info 
Y332(10.83)  LDD3495  [3]
Acrolein
 Probe Info 
N.A.  LDD0222  [4]
5E-2FA
 Probe Info 
N.A.  LDD2235  [5]
m-APA
 Probe Info 
N.A.  LDD2231  [5]
1c-yne
 Probe Info 
N.A.  LDD0228  [6]
PAL-AfBPP Probe
Click To Hide/Show 35 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C022
 Probe Info 
6.92  LDD1728  [7]
C040
 Probe Info 
9.13  LDD1740  [7]
C041
 Probe Info 
5.62  LDD1741  [7]
C045
 Probe Info 
4.92  LDD1744  [7]
C053
 Probe Info 
6.87  LDD1751  [7]
C063
 Probe Info 
10.13  LDD1760  [7]
C106
 Probe Info 
23.43  LDD1793  [7]
C107
 Probe Info 
6.23  LDD1794  [7]
C108
 Probe Info 
8.57  LDD1795  [7]
C149
 Probe Info 
5.13  LDD1830  [7]
C153
 Probe Info 
19.84  LDD1834  [7]
C159
 Probe Info 
8.28  LDD1839  [7]
C170
 Probe Info 
13.45  LDD1850  [7]
C186
 Probe Info 
8.11  LDD1864  [7]
C197
 Probe Info 
6.41  LDD1873  [7]
C201
 Probe Info 
25.81  LDD1877  [7]
C208
 Probe Info 
7.67  LDD1883  [7]
C211
 Probe Info 
9.19  LDD1885  [7]
C220
 Probe Info 
13.45  LDD1894  [7]
C221
 Probe Info 
6.11  LDD1895  [7]
C223
 Probe Info 
6.59  LDD1897  [7]
C237
 Probe Info 
5.74  LDD1910  [7]
C264
 Probe Info 
18.77  LDD1935  [7]
C277
 Probe Info 
8.22  LDD1947  [7]
C281
 Probe Info 
6.77  LDD1951  [7]
C310
 Probe Info 
12.73  LDD1977  [7]
C349
 Probe Info 
10.20  LDD2010  [7]
C350
 Probe Info 
46.85  LDD2011  [7]
C356
 Probe Info 
8.06  LDD2017  [7]
C376
 Probe Info 
7.36  LDD2036  [7]
C386
 Probe Info 
7.01  LDD2045  [7]
C390
 Probe Info 
34.06  LDD2049  [7]
C425
 Probe Info 
11.47  LDD2080  [7]
C429
 Probe Info 
11.16  LDD2084  [7]
OEA-DA
 Probe Info 
14.01  LDD0046  [8]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [4]
 LDCM0109  NEM HeLa N.A.  LDD0225  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858

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 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
2 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
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 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
5 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
6 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.
7 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
8 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570