Details of the Target

General Information of Target

Target ID LDTP02350
Target Name Glutathione S-transferase Mu 1 (GSTM1)
Gene Name GSTM1
Gene ID 2944
Synonyms
GST1; Glutathione S-transferase Mu 1; EC 2.5.1.18; GST HB subunit 4; GST class-mu 1; GSTM1-1; GSTM1a-1a; GSTM1b-1b; GTH4
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPMILGYWDIRGLAHAIRLLLEYTDSSYEEKKYTMGDAPDYDRSQWLNEKFKLGLDFPNL
PYLIDGAHKITQSNAILCYIARKHNLCGETEEEKIRVDILENQTMDNHMQLGMICYNPEF
EKLKPKYLEELPEKLKLYSEFLGKRPWFAGNKITFVDFLVYDVLDLHRIFEPKCLDAFPN
LKDFISRFEGLEKISAYMKSSRFLPRPVFSKMAVWGNK
Target Bioclass
Enzyme
Family
GST superfamily, Mu family
Subcellular location
Cytoplasm
Function
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Involved in the formation of glutathione conjugates of both prostaglandin A2 (PGA2) and prostaglandin J2 (PGJ2). Participates in the formation of novel hepoxilin regioisomers.
Uniprot ID
P09488
Ensemble ID
ENST00000309851.10
HGNC ID
HGNC:4632
ChEMBL ID
CHEMBL2081

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CHL1 SNV: p.R18C .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 12 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
CY4
 Probe Info  		100.00  LDD0244  [1]
TH211
 Probe Info  		Y62(20.00); Y197(5.53)  LDD0260  [2]
STPyne
 Probe Info  		K211(0.89)  LDD0277  [3]
Probe 1
 Probe Info  		Y41(17.98)  LDD3495  [4]
BTD
 Probe Info  		C174(0.49)  LDD2104  [5]
Jackson_1
 Probe Info  		3.33  LDD0120  [6]
IPM
 Probe Info  		C174(6.61)  LDD1702  [5]
4-Iodoacetamidophenylacetylene
 Probe Info  		C174(0.00); C87(0.00); C78(0.00)  LDD0038  [7]
IA-alkyne
 Probe Info  		C174(0.00); C87(0.00); C78(0.00); C115(0.00)  LDD0036  [7]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [8]
Lodoacetamide azide
 Probe Info  		C115(0.00); C78(0.00); C174(0.00); C87(0.00)  LDD0037  [7]
NAIA_5
 Probe Info  		C87(0.00); C78(0.00)  LDD2223  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0070  Cisar_cp37 MDA-MB-231 3.33  LDD0120  [6]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C174(6.61)  LDD1702  [5]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C174(0.49)  LDD2104  [5]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C174(0.32)  LDD2114  [5]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acetaminophen Small molecular drug DB00316
Amitriptyline Small molecular drug DB00321
Azathioprine Small molecular drug DB00993
Chloroquine Small molecular drug DB00608
Cisplatin Small molecular drug DB00515
Curcumin Small molecular drug DB11672
Deoxycholic Acid Small molecular drug DB03619
Glutathione Small molecular drug DB00143
Glutathione Disulfide Small molecular drug DB03310
Isosorbide Mononitrate Small molecular drug DB01020
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(9r10r)-9-(S-glutathionyl)-10-hydroxy-910-dihydrophenanthrene . DB01834
(9s10s)-9-(S-glutathionyl)-10-hydroxy-910-dihydrophenanthrene . DB04187
5-fluorotryptophan . DB03314
S-(24-dinitrophenyl)Glutathione . DB02458
Zinc Trihydroxide . DB02165

References

1 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
2 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.
3 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
4 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.
5 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
6 Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide. J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.
7 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
8 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
9 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