Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT5MLC4)

DTT Name Leukocyte proteinase-3 (PRTN3)
Synonyms Wegener autoantigen; PR3; PR-3; P29; Neutrophil proteinase 4; NP4; NP-4; Myeloblastin; MBN; Leukocyte proteinase 3; CANCA antigen; C-ANCA antigen; AGP7
Gene Name PRTN3
DTT Type
Clinical trial target
 [1]
BioChemical Class
Peptidase
UniProt ID
PRTN3_HUMAN
TTD ID
T15882
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 3.4.21.76
Sequence
MAHRPPSPALASVLLALLLSGAARAAEIVGGHEAQPHSRPYMASLQMRGNPGSHFCGGTL
IHPSFVLTAAHCLRDIPQRLVNVVLGAHNVRTQEPTQQHFSVAQVFLNNYDAENKLNDVL
LIQLSSPANLSASVATVQLPQQDQPVPHGTQCLAMGWGRVGAHDPPAQVLQELNVTVVTF
FCRPHNICTFVPRRKAGICFGDSGGPLICDGIIQGIDSFVIWGCATRLFPDFFTRVALYV
DWIRSTLRRVEAKGRP
Function
By cleaving and activating receptor F2RL1/PAR-2, enhances endothelial cell barrier function and thus vascular integrity during neutrophil transendothelial migration. May play a role in neutrophil transendothelial migration, probably when associated with CD177. Serine protease that degrades elastin, fibronectin, laminin, vitronectin, and collagen types I, III, and IV (in vitro).
Reactome Pathway
Common Pathway of Fibrin Clot Formation (R-HSA-140875 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
2 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Combined PR1/WT1 vaccine DMGCTX5 Myeloid leukaemia 2B33.1 Phase 2 [1]
Tiprelestat DM1SB94 Myocardial infarction BA41-BA43 Phase 2 [2]
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1 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID22595175C4g DM9SLUK Discovery agent N.A. Investigative [3]
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Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Acute myelocytic leukaemia 2C82 Bone marrow 1.98E-40 -2.04 -1.63
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References

1 Leukemia-associated antigen-specific T-cell responses following combined PR1 and WT1 peptide vaccination in patients with myeloid malignancies. Blood. 2008 Jan 1;111(1):236-42.
2 Company report (Proteo Biotech AG)
3 N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3993-7.