Target Information
Target General Infomation | |||||
---|---|---|---|---|---|
Target ID |
T22839
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Former ID |
TTDR00230
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Target Name |
Elastase 1
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Gene Name |
CELA1
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Synonyms |
Elastase; CELA1
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Target Type |
Successful
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Disease | Alpha-1 antitrypsin deficiency [ICD9: 273.4; ICD10: E88.0] | ||||
Bronchitis [ICD10: J20-J21, J42] | |||||
Cystic fibrosis [ICD9: 277; ICD10: E84] | |||||
Chronic obstructive pulmonary disease [ICD9: 490-492, 494-496; ICD10: J40-J44, J47] | |||||
Emphysema [ICD9: 492; ICD10: J43] | |||||
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25] | |||||
Function |
Acts upon elastin.
|
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BioChemical Class |
Peptidase
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Target Validation |
T22839
|
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UniProt ID | |||||
EC Number |
EC 3.4.21.36
|
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Sequence |
MLVLYGHSTQDLPETNARVVGGTEAGRNSWPSQISLQYRSGGSRYHTCGGTLIRQNWVMT
AAHCVDYQKTFRVVAGDHNLSQNDGTEQYVSVQKIVVHPYWNSDNVAAGYDIALLRLAQS VTLNSYVQLGVLPQEGAILANNSPCYITGWGKTKTNGQLAQTLQQAYLPSVDYAICSSSS YWGSTVKNTMVCAGGDGVRSGCQGDSGGPLHCLVNGKYSVHGVTSFVSSRGCNVSRKPTV FTQVSAYISWINNVIASN |
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Drugs and Mode of Action | |||||
Drug(s) | Alpha 1-PI | Drug Info | Approved | Alpha-1 antitrypsin deficiency | [545546], [551871] |
Erdosteine | Drug Info | Approved | Bronchitis | [551871] | |
Sivelestat | Drug Info | Phase 4 | Discovery agent | [521724], [541582] | |
Mdl 101,146 | Drug Info | Terminated | Inflammatory disease | [546375] | |
PBI-1101 | Drug Info | Terminated | Inflammatory disease | [547638] | |
SSR-69071 | Drug Info | Terminated | Chronic obstructive pulmonary disease | [547262] | |
SYN-1134 | Drug Info | Terminated | Cystic fibrosis | [547708] | |
WIN-63759 | Drug Info | Terminated | Emphysema | [546320] | |
Inhibitor | (2-BROMOETHYL)(2-'FORMYL-4'-AMINOPHENYL) ACETATE | Drug Info | [551374] | ||
(Tert-Butyloxycarbonyl)-Alanyl-Alanyl-Amine | Drug Info | [551393] | |||
Acetate Ion | Drug Info | [551393] | |||
Acetyl-Ala-Ala-Pro-Ala-trifluromethane | Drug Info | [532036] | |||
Acetyl-Pro-Ala-Pro-Ala-trifluoro methane | Drug Info | [532036] | |||
Alpha 1-PI | Drug Info | [535306] | |||
Dimethylformamide | Drug Info | [551397] | |||
GRASSYSTATIN A | Drug Info | [530345] | |||
Mdl 101,146 | Drug Info | [551393] | |||
MOLASSAMIDE | Drug Info | [530586] | |||
Para-Isopropylaniline | Drug Info | [551393] | |||
PBI-1101 | Drug Info | [550871] | |||
Sivelestat | Drug Info | [537405] | |||
SSR-69071 | Drug Info | [531528] | |||
SYN-1134 | Drug Info | [550874] | |||
Modulator | Erdosteine | Drug Info | [551871] | ||
WIN-63759 | Drug Info | [550030] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
References | |||||
Ref 521724 | ClinicalTrials.gov (NCT00219375) Study of Sivelestat Sodium Hydrate in Acute Lung Injury (ALI) Associated With Systemic Inflammatory Response Syndrome (SIRS) in Japan. U.S. National Institutes of Health. | ||||
Ref 541582 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6441). | ||||
Ref 545546 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003666) | ||||
Ref 546320 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007449) | ||||
Ref 546375 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007771) | ||||
Ref 547262 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014569) | ||||
Ref 547638 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018032) | ||||
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 530586 | J Nat Prod. 2010 Mar 26;73(3):459-62.Molassamide, a depsipeptide serine protease inhibitor from the marine cyanobacterium Dichothrix utahensis. | ||||
Ref 531528 | Pivotal role for alpha1-antichymotrypsin in skin repair. J Biol Chem. 2011 Aug 19;286(33):28889-901. | ||||
Ref 532036 | J Med Chem. 1990 Jan;33(1):394-407.Synthesis of peptidyl fluoromethyl ketones and peptidyl alpha-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and humanneutrophil cathepsin G. | ||||
Ref 537405 | Sivelestat (selective neutrophil elastase inhibitor) improves the mortality rate of sepsis associated with both ARDS and DIC patients. Shock. 2009 May 18. | ||||
Ref 550030 | Biological activity of WIN 63759, an orally bioavailable inhibitor of human neutrophil elastase. Drug Development Research Volume 34, Issue 3, pages 306-316, March 1995. | ||||
Ref 550871 | CN patent application no. 1813706, Use of elastic protease inhibitor for preparing medicine for protecting cerebral hemorrhage. | ||||
Ref 550874 | EP patent application no. 1292314, Method for treating respiratory disorders associated with pulmonary elastic fiber injury comprising the use of glycosaminoglycans. |
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