General Information of Drug Therapeutic Target (DTT) (ID: TTPTWV5)

DTT Name Legumain (LGMN)
Synonyms Protease, cysteine 1; PRSC1; Asparaginyl endopeptidase
Gene Name LGMN
DTT Type
Clinical trial target
[1]
BioChemical Class
Peptidase
UniProt ID
LGMN_HUMAN
TTD ID
T32973
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 3.4.22.34
Sequence
MVWKVAVFLSVALGIGAVPIDDPEDGGKHWVVIVAGSNGWYNYRHQADACHAYQIIHRNG
IPDEQIVVMMYDDIAYSEDNPTPGIVINRPNGTDVYQGVPKDYTGEDVTPQNFLAVLRGD
AEAVKGIGSGKVLKSGPQDHVFIYFTDHGSTGILVFPNEDLHVKDLNETIHYMYKHKMYR
KMVFYIEACESGSMMNHLPDNINVYATTAANPRESSYACYYDEKRSTYLGDWYSVNWMED
SDVEDLTKETLHKQYHLVKSHTNTSHVMQYGNKTISTMKVMQFQGMKRKASSPVPLPPVT
HLDLTPSPDVPLTIMKRKLMNTNDLEESRQLTEEIQRHLDARHLIEKSVRKIVSLLAASE
AEVEQLLSERAPLTGHSCYPEALLHFRTHCFNWHSPTYEYALRHLYVLVNLCEKPYPLHR
IKLSMDHVCLGHY
Function
Can also cleave aspartyl bonds slowly, especially under acidic conditions. Required for normal lysosomal protein degradation in renal proximal tubules. Required for normal degradation of internalized EGFR. Plays a role in the regulation of cell proliferation via its role in EGFR degradation. May be involved in the processing of proteins for MHC class II antigen presentation in the lysosomal/endosomal system. Has a strict specificity for hydrolysis of asparaginyl bonds.
KEGG Pathway
Lysosome (hsa04142 )
Antigen processing and presentation (hsa04612 )
Reactome Pathway
Vitamin D (calciferol) metabolism (R-HSA-196791 )
MHC class II antigen presentation (R-HSA-2132295 )
Trafficking and processing of endosomal TLR (R-HSA-1679131 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
1 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Legumain-cleavable doxorubicin prodrugs DMEUGZL Solid tumour/cancer 2A00-2F9Z Phase 2/3 [1]
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1 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID24775305C7u DMDMU01 Discovery agent N.A. Investigative [2]
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References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2380).
2 P3 SAR exploration of biphenyl carbamate based Legumain inhibitors. Bioorg Med Chem Lett. 2014 Jun 1;24(11):2521-4.