Target Information
Target General Infomation | |||||
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Target ID |
T14558
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Former ID |
TTDS00130
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Target Name |
Tryptase
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Gene Name |
TPSAB1
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Synonyms |
Tryptase I; Tryptase alpha-1; Tryptase alpha/beta-1; TPSAB1
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Target Type |
Successful
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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
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Target Validation |
T14558
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UniProt ID | |||||
EC Number |
EC 3.4.21.59
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Sequence |
MLNLLLLALPVLASRAYAAPAPGQALQRVGIVGGQEAPRSKWPWQVSLRVHGPYWMHFCG
GSLIHPQWVLTAAHCVGPDVKDLAALRVQLREQHLYYQDQLLPVSRIIVHPQFYTAQIGA DIALLELEEPVNVSSHVHTVTLPPASETFPPGMPCWVTGWGDVDNDERLPPPFPLKQVKV PIMENHICDAKYHLGAYTGDDVRIVRDDMLCAGNTRRDSCQGDSGGPLVCKVNGTWLQAG VVSWGEGCAQPNRPGIYTRVTYYLDWIHHYVPKKP |
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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Pentamidine | Drug Info | Withdrawn from market | Human immunodeficiency virus infection | [551871] | |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 | |||||
References | |||||
Ref 536135 | Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. | ||||
Ref 545523 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003595) | ||||
Ref 546389 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007862) | ||||
Ref 546732 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010022) | ||||
Ref 546785 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010270) | ||||
Ref 526283 | 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. | ||||
Ref 526439 | Bioorg Med Chem Lett. 2002 Nov 4;12(21):3229-33.Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. | ||||
Ref 530345 | J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. | ||||
Ref 534849 | Inhibitors of tryptase for the treatment of mast cell-mediated diseases. Curr Pharm Des. 1998 Oct;4(5):381-96. | ||||
Ref 535361 | Tryptase inhibition blocks airway inflammation in a mouse asthma model. J Immunol. 2002 Feb 15;168(4):1992-2000. | ||||
Ref 537936 | Bis(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. |
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