Target Information

Target General Infomation
Target ID
T14558
Former ID
TTDS00130
Target Name
Tryptase
Gene Name
TPSAB1
Synonyms
Tryptase I; Tryptase alpha-1; Tryptase alpha/beta-1; TPSAB1
Target Type
Successful
Disease Asthma [ICD10: J45]
Fungal infections [ICD9: 110-118; ICD10: B35-B49]
Human immunodeficiency virus infection [ICD9: 279.3; ICD10: B20-B26]
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
BioChemical Class
Peptidase
Target Validation
T14558
UniProt ID
Q15661
EC Number
EC 3.4.21.59
Sequence
MLNLLLLALPVLASRAYAAPAPGQALQRVGIVGGQEAPRSKWPWQVSLRVHGPYWMHFCG
GSLIHPQWVLTAAHCVGPDVKDLAALRVQLREQHLYYQDQLLPVSRIIVHPQFYTAQIGA
DIALLELEEPVNVSSHVHTVTLPPASETFPPGMPCWVTGWGDVDNDERLPPPFPLKQVKV
PIMENHICDAKYHLGAYTGDDVRIVRDDMLCAGNTRRDSCQGDSGGPLVCKVNGTWLQAG
VVSWGEGCAQPNRPGIYTRVTYYLDWIHHYVPKKP
Drugs and Mode of Action
Drug(s) Lactoferrin Drug Info Approved Solid tumours [551871]
Pentamidine Drug Info Approved Fungal infections [536135]
Pentamidine Drug Info Withdrawn from market Human immunodeficiency virus infection [551871]
APC-2059 Drug Info Discontinued in Phase 2 Inflammatory bowel disease [546785]
APC-366 Drug Info Discontinued in Phase 2 Asthma [545523]
BABIM Drug Info Terminated Asthma [546732]
BAY-17-1998 Drug Info Terminated Asthma [546389]
BAY-44-3428 Drug Info Terminated Asthma [546878]
Inhibitor Actoferrin Drug Info [534849]
AMG-126737 Drug Info [535361]
APC-2059 Drug Info [526283]
APC-366 Drug Info [534849]
BABIM Drug Info [534849]
BAY-44-3428 Drug Info [551726]
BMS-262084 Drug Info [526439]
GRASSYSTATIN A Drug Info [530345]
Lactoferrin Drug Info [534849]
MOL 6131 Drug Info [535361]
Pentamidine Drug Info [534849], [537936]
Modulator BAY-17-1998 Drug Info [551727]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
Reactome Activation of Matrix Metalloproteinases
References
Ref 536135Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40.
Ref 545523Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003595)
Ref 546389Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007862)
Ref 546732Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010022)
Ref 546785Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010270)
Ref 546878Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010843)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 526283Treatment 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.
Ref 526439Bioorg Med Chem Lett. 2002 Nov 4;12(21):3229-33.Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.
Ref 530345J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
Ref 534849Inhibitors of tryptase for the treatment of mast cell-mediated diseases. Curr Pharm Des. 1998 Oct;4(5):381-96.
Ref 535361Tryptase inhibition blocks airway inflammation in a mouse asthma model. J Immunol. 2002 Feb 15;168(4):1992-2000.
Ref 537936Bis(5-amidino-2-benzimidazolyl)methane and related amidines are potent, reversible inhibitors of mast cell tryptases. J Pharmacol Exp Ther. 1993 Feb;264(2):676-82.
Ref 551726Bayer AG to Develop Arris Asthma Compound; Arris to Receive Milestone Payment. 1996 Business Wire
Ref 551727Bayer AG to Develop Arris Asthma Compound; Arris to Receive Milestone Payment. 1996 Business Wire

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