Details of the Target

General Information of Target

Target ID LDTP05548
Target Name Protein-glutamine gamma-glutamyltransferase E (TGM3)
Gene Name TGM3
Gene ID 7053
Synonyms
Protein-glutamine gamma-glutamyltransferase E; EC 2.3.2.13; Transglutaminase E; TG(E); TGE; TGase E; Transglutaminase-3; TGase-3) [Cleaved into: Protein-glutamine gamma-glutamyltransferase E 50 kDa catalytic chain; Protein-glutamine gamma-glutamyltransferase E 27 kDa non-catalytic chain]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAALGVQSINWQTAFNRQAHHTDKFSSQELILRRGQNFQVLMIMNKGLGSNERLEFIVST
GPYPSESAMTKAVFPLSNGSSGGWSAVLQASNGNTLTISISSPASAPIGRYTMALQIFSQ
GGISSVKLGTFILLFNPWLNVDSVFMGNHAEREEYVQEDAGIIFVGSTNRIGMIGWNFGQ
FEEDILSICLSILDRSLNFRRDAATDVASRNDPKYVGRVLSAMINSNDDNGVLAGNWSGT
YTGGRDPRSWNGSVEILKNWKKSGFSPVRYGQCWVFAGTLNTALRSLGIPSRVITNFNSA
HDTDRNLSVDVYYDPMGNPLDKGSDSVWNFHVWNEGWFVRSDLGPSYGGWQVLDATPQER
SQGVFQCGPASVIGVREGDVQLNFDMPFIFAEVNADRITWLYDNTTGKQWKNSVNSHTIG
RYISTKAVGSNARMDVTDKYKYPEGSDQERQVFQKALGKLKPNTPFAATSSMGLETEEQE
PSIIGKLKVAGMLAVGKEVNLVLLLKNLSRDTKTVTVNMTAWTIIYNGTLVHEVWKDSAT
MSLDPEEEAEHPIKISYAQYEKYLKSDNMIRITAVCKVPDESEVVVERDIILDNPTLTLE
VLNEARVRKPVNVQMLFSNPLDEPVRDCVLMVEGSGLLLGNLKIDVPTLGPKEGSRVRFD
ILPSRSGTKQLLADFSCNKFPAIKAMLSIDVAE
Target Bioclass
Enzyme
Family
Transglutaminase superfamily, Transglutaminase family
Subcellular location
Cytoplasm
Function
Catalyzes the calcium-dependent formation of isopeptide cross-links between glutamine and lysine residues in various proteins, as well as the conjugation of polyamines to proteins. Involved in the formation of the cornified envelope (CE), a specialized component consisting of covalent cross-links of proteins beneath the plasma membrane of terminally differentiated keratinocytes. Catalyzes small proline-rich proteins (SPRR1 and SPRR2) and LOR cross-linking to form small interchain oligomers, which are further cross-linked by TGM1 onto the growing CE scaffold. In hair follicles, involved in cross-linking structural proteins to hardening the inner root sheath.
Uniprot ID
Q08188
Ensemble ID
ENST00000381458.6
HGNC ID
HGNC:11779
ChEMBL ID
CHEMBL3363

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C367(1.52); C273(1.48)  LDD2252  [1]
NAIA_4
 Probe Info  		N.A.  LDD2226  [2]
YN-1
 Probe Info  		N.A.  LDD0447  [3]
PAL-AfBPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe12
 Probe Info  		20.00  LDD0474  [4]
FFF probe9
 Probe Info  		20.00  LDD0470  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A204 C367(1.52); C273(1.48)  LDD2252  [1]
 LDCM0023  KB03 A204 C677(1.37)  LDD2669  [1]
 LDCM0024  KB05 A204 C367(1.23)  LDD3086  [1]

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
L-glutamine Small molecular drug DB00130
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
5'-guanosine-diphosphate-monothiophosphate Small molecular drug DB01864
B-2-octylglucoside Small molecular drug DB03152
Guanosine-5'-diphosphate Small molecular drug DB04315
Guanosine-5'-monophosphate Small molecular drug DB01972

References

1 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
2 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
3 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
4 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.