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 | |||||
| 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 | [1] |
| Pentamidine | Drug Info | Approved | Fungal infections | [2] | |
| Pentamidine | Drug Info | Withdrawn from market | Human immunodeficiency virus infection | [1] | |
| APC-2059 | Drug Info | Discontinued in Phase 2 | Inflammatory bowel disease | [3] | |
| APC-366 | Drug Info | Discontinued in Phase 2 | Asthma | [4] | |
| BABIM | Drug Info | Terminated | Asthma | [5] | |
| BAY-17-1998 | Drug Info | Terminated | Asthma | [6] | |
| BAY-44-3428 | Drug Info | Terminated | Asthma | [7] | |
| Inhibitor | Actoferrin | Drug Info | [8] | ||
| AMG-126737 | Drug Info | [9] | |||
| APC-2059 | Drug Info | [10] | |||
| APC-366 | Drug Info | [8] | |||
| BABIM | Drug Info | [8] | |||
| BAY-44-3428 | Drug Info | [11] | |||
| BMS-262084 | Drug Info | [12] | |||
| GRASSYSTATIN A | Drug Info | [13] | |||
| Lactoferrin | Drug Info | [8] | |||
| MOL 6131 | Drug Info | [9] | |||
| Pentamidine | Drug Info | [8], [14] | |||
| Modulator | BAY-17-1998 | Drug Info | [15] | ||
| Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
| TEP | EXP Info | ||||
| Pathways | |||||
| Reactome | Activation of Matrix Metalloproteinases | ||||
| References | |||||
| REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 2 | Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. | ||||
| REF 3 | 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 4 | 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 5 | 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 6 | 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 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010843) | ||||
| REF 8 | Inhibitors of tryptase for the treatment of mast cell-mediated diseases. Curr Pharm Des. 1998 Oct;4(5):381-96. | ||||
| REF 9 | Tryptase inhibition blocks airway inflammation in a mouse asthma model. J Immunol. 2002 Feb 15;168(4):1992-2000. | ||||
| REF 10 | 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 11 | Bayer AG to Develop Arris Asthma Compound; Arris to Receive Milestone Payment. 1996 Business Wire | ||||
| REF 12 | Bioorg Med Chem Lett. 2002 Nov 4;12(21):3229-33.Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. | ||||
| REF 13 | 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 14 | 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. | ||||
| REF 15 | Bayer AG to Develop Arris Asthma Compound; Arris to Receive Milestone Payment. 1996 Business Wire | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.