Details of the Target

General Information of Target

Target ID LDTP12784
Target Name Pyroglutamyl-peptidase 1 (PGPEP1)
Gene Name PGPEP1
Gene ID 54858
Synonyms
PGPI; Pyroglutamyl-peptidase 1; EC 3.4.19.3; 5-oxoprolyl-peptidase; Pyroglutamyl aminopeptidase I; PAP-I; Pyroglutamyl-peptidase I; PGP-I; Pyrrolidone-carboxylate peptidase
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MACTKTLQQSQPISAGATTTTTAVAPAGGHSGSTECDLECLVCREPYSCPRLPKLLACQH
AFCAICLKLLLCVQDNTWSITCPLCRKVTAVPGGLICSLRDHEAVVGQLAQPCTEVSLCP
QGLVDPADLAAGHPSLVGEDGQDEVSANHVAARRLAAHLLLLALLIILIGPFIYPGVLRW
VLTFIIALALLMSTLFCCLPSTRGSCWPSSRTLFCREQKHSHISSIA
Target Bioclass
Enzyme
Family
Peptidase C15 family
Subcellular location
Cytoplasm
Function Removes 5-oxoproline from various penultimate amino acid residues except L-proline.
Uniprot ID
Q9NXJ5
Ensemble ID
ENST00000252813.5
HGNC ID
HGNC:13568

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
JURKAT SNV: p.R183K .
MFE319 SNV: p.T152A DBIA    Probe Info 
RCC10RGB SNV: p.Q142R .
RKO SNV: p.Ter210RextTer147 DBIA    Probe Info 

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
DBIA
 Probe Info  		C99(12.16)  LDD0209  [1]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [2]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [2]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [2]
IPM
 Probe Info  		N.A.  LDD0025  [3]
NAIA_4
 Probe Info  		N.A.  LDD2226  [4]
NAIA_5
 Probe Info  		C206(0.00); C87(0.00)  LDD2223  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0630  CCW28-3 231MFP C149(1.37)  LDD2214  [5]
 LDCM0632  CL-Sc Hep-G2 C206(20.00); C149(0.72); C206(0.31); C87(0.19)  LDD2227  [4]
 LDCM0198  Dimethyl Fumarate(DMF) T cell C149(7.50)  LDD0513  [6]
 LDCM0201  EV-3 T cell C149(6.29)  LDD0515  [6]
 LDCM0202  EV-93 T cell C149(5.00)  LDD0527  [6]
 LDCM0572  Fragment10 Ramos C149(11.02)  LDD1466  [7]
 LDCM0573  Fragment11 Ramos C149(1.31)  LDD2190  [8]
 LDCM0574  Fragment12 MDA-MB-231 C149(3.93)  LDD1468  [7]
 LDCM0575  Fragment13 Ramos C149(20.00)  LDD1470  [7]
 LDCM0576  Fragment14 Ramos C149(0.91)  LDD2193  [8]
 LDCM0566  Fragment4 MDA-MB-231 C149(20.00)  LDD1461  [7]
 LDCM0569  Fragment7 Ramos C149(1.32)  LDD2186  [8]
 LDCM0571  Fragment9 Ramos C149(20.00)  LDD1464  [7]
 LDCM0022  KB02 T cell C149(17.69)  LDD1703  [6]
 LDCM0023  KB03 Jurkat C99(12.16)  LDD0209  [1]
 LDCM0024  KB05 COLO792 C99(1.65)  LDD3310  [9]
 LDCM0169  KB63 Ramos 20.00  LDD0432  [10]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein N-terminal glutamine amidohydrolase (NTAQ1) NTAQ1 family Q96HA8
Ubiquitin-conjugating enzyme E2 E2 (UBE2E2) Ubiquitin-conjugating enzyme family Q96LR5
Ubiquitin-conjugating enzyme E2 E3 (UBE2E3) Ubiquitin-conjugating enzyme family Q969T4
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Aquaporin-1 (AQP1) MIP/aquaporin (TC 1.A.8) family P29972

References

1 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
2 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
3 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
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 Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. doi: 10.1021/acschembio.8b01083. Epub 2019 May 13.
6 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
7 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
8 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578
9 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
10 2-Sulfonylpyridines as Tunable, Cysteine-Reactive Electrophiles. J Am Chem Soc. 2020 May 13;142(19):8972-8979. doi: 10.1021/jacs.0c02721. Epub 2020 Apr 29.