Target Information
| Target General Information | Top | |||||
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| Target ID |
T14558
(Former ID: TTDS00130)
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| Target Name |
Tryptase alpha/beta-1 (Tryptase)
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| Synonyms |
Tryptase-1; Tryptase alpha-1; Tryptase I; TPSB1; TPS2; TPS1
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| Gene Name |
TPSAB1
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Fungal infection [ICD-11: 1F29-1F2F] | |||||
| 2 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| 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.
Click to Show/Hide
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| BioChemical Class |
Peptidase
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| UniProt ID | ||||||
| EC Number |
EC 3.4.21.59
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| Sequence |
MLNLLLLALPVLASRAYAAPAPGQALQRVGIVGGQEAPRSKWPWQVSLRVHGPYWMHFCG
GSLIHPQWVLTAAHCVGPDVKDLAALRVQLREQHLYYQDQLLPVSRIIVHPQFYTAQIGA DIALLELEEPVNVSSHVHTVTLPPASETFPPGMPCWVTGWGDVDNDERLPPPFPLKQVKV PIMENHICDAKYHLGAYTGDDVRIVRDDMLCAGNTRRDSCQGDSGGPLVCKVNGTWLQAG VVSWGEGCAQPNRPGIYTRVTYYLDWIHHYVPKKP Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Lactoferrin | Drug Info | Approved | Solid tumour/cancer | [2] | |
| 2 | Pentamidine | Drug Info | Approved | Fungal infection | [3] | |
| Discontinued Drug(s) | [+] 5 Discontinued Drugs | + | ||||
| 1 | APC-2059 | Drug Info | Discontinued in Phase 2 | Inflammatory bowel disease | [4] | |
| 2 | APC-366 | Drug Info | Discontinued in Phase 2 | Asthma | [5] | |
| 3 | BABIM | Drug Info | Terminated | Asthma | [6] | |
| 4 | BAY-17-1998 | Drug Info | Terminated | Asthma | [7] | |
| 5 | BAY-44-3428 | Drug Info | Terminated | Asthma | [8] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 11 Inhibitor drugs | + | ||||
| 1 | Lactoferrin | Drug Info | [1] | |||
| 2 | Pentamidine | Drug Info | [1], [9] | |||
| 3 | APC-2059 | Drug Info | [10] | |||
| 4 | APC-366 | Drug Info | [1] | |||
| 5 | BABIM | Drug Info | [1] | |||
| 6 | BAY-44-3428 | Drug Info | [12] | |||
| 7 | AMG-126737 | Drug Info | [13] | |||
| 8 | BMS-262084 | Drug Info | [14] | |||
| 9 | Grassystatin a | Drug Info | [15] | |||
| 10 | Lactoferrin | Drug Info | [1] | |||
| 11 | MOL 6131 | Drug Info | [13] | |||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | BAY-17-1998 | Drug Info | [11] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| Reactome | [+] 1 Reactome Pathways | + | ||||
| 1 | Activation of Matrix Metalloproteinases | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | Inhibitors of tryptase for the treatment of mast cell-mediated diseases. Curr Pharm Des. 1998 Oct;4(5):381-96. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. | |||||
| 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 800010270) | |||||
| 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 800003595) | |||||
| 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 800010022) | |||||
| 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 800007862) | |||||
| REF 8 | 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 9 | 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 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 | Bayer AG to Develop Arris Asthma Compound; Arris to Receive Milestone Payment. 1996 Business Wire | |||||
| REF 13 | Tryptase inhibition blocks airway inflammation in a mouse asthma model. J Immunol. 2002 Feb 15;168(4):1992-2000. | |||||
| REF 14 | Synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3229-33. | |||||
| REF 15 | Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. J Med Chem. 2009 Sep 24;52(18):5732-47. | |||||
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