Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTM1TDX)

DTT Name	Tryptase alpha/beta-1 (Tryptase)
Synonyms	Tryptase-1; Tryptase alpha-1; Tryptase I; TPSB1; TPS2; TPS1
Gene Name	TPSAB1
DTT Type	Successful target	[1]
BioChemical Class	Peptidase
UniProt ID	TRYB1_HUMAN
TTD ID	T14558
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
EC Number	EC 3.4.21.59
Sequence	MLNLLLLALPVLASRAYAAPAPGQALQRVGIVGGQEAPRSKWPWQVSLRVHGPYWMHFCG GSLIHPQWVLTAAHCVGPDVKDLAALRVQLREQHLYYQDQLLPVSRIIVHPQFYTAQIGA DIALLELEEPVNVSSHVHTVTLPPASETFPPGMPCWVTGWGDVDNDERLPPPFPLKQVKV PIMENHICDAKYHLGAYTGDDVRIVRDDMLCAGNTRRDSCQGDSGGPLVCKVNGTWLQAG VVSWGEGCAQPNRPGIYTRVTYYLDWIHHYVPKKP
Function	May play a role in innate immunity. Isoform 2 cleaves large substrates, such as fibronectin, more efficiently than isoform 1, but seems less efficient toward small substrates. Tryptase is the major neutral protease present in mast cells and is secreted upon the coupled activation-degranulation response of this cell type.
KEGG Pathway	Influenza A (hsa05164 )
Reactome Pathway	Activation of Matrix Metalloproteinases (R-HSA-1592389 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA)

Jump to Detail Molecular Interaction Atlas of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Lactoferrin	DMA7QTC	Solid tumour/cancer	2A00-2F9Z	Approved	[1]
Pentamidine	DMHZJCG	African trypanosomiasis	1F51	Approved	[1]
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5 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
APC-2059	DM8IB6K	Inflammatory bowel disease	DD72	Discontinued in Phase 2	[2]
APC-366	DM02DNQ	Asthma	CA23	Discontinued in Phase 2	[1]
BABIM	DM8AGOE	Asthma	CA23	Terminated	[1]
BAY-17-1998	DM7LZFQ	Asthma	CA23	Terminated	[3]
BAY-44-3428	DM40ORU	Asthma	CA23	Terminated	[4]
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4 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AMG-126737	DM9H7AZ	Discovery agent	N.A.	Investigative	[5]
BMS-262084	DMETNA3	Discovery agent	N.A.	Investigative	[6]
Grassystatin a	DM1PWX2	Discovery agent	N.A.	Investigative	[7]
MOL 6131	DMSF8UC	Discovery agent	N.A.	Investigative	[5]
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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
Asthma	CA23	Nasal and bronchial airway	3.09E-07	1.07	0.89
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References

1	Inhibitors of tryptase for the treatment of mast cell-mediated diseases. Curr Pharm Des. 1998 Oct;4(5):381-96.
2	Treatment of mildly to moderately active ulcerative colitis with a tryptase inhibitor (APC 2059): an open-label pilot study. Aliment Pharmacol Ther. 2002 Mar;16(3):407-13.
3	Bayer AG to Develop Arris Asthma Compound; Arris to Receive Milestone Payment. 1996 Business Wire
4	Bayer AG to Develop Arris Asthma Compound; Arris to Receive Milestone Payment. 1996 Business Wire
5	Tryptase inhibition blocks airway inflammation in a mouse asthma model. J Immunol. 2002 Feb 15;168(4):1992-2000.
6	Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3229-33.
7	Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47.