Target Information

Target General Infomation
Target ID
T22839
Former ID
TTDR00230
Target Name
Elastase 1
Gene Name
CELA1
Synonyms
Elastase; CELA1
Target Type
Successful
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.
BioChemical Class
Peptidase
Target Validation
T22839
UniProt ID
Q9UNI1
EC Number
EC 3.4.21.36
Sequence
MLVLYGHSTQDLPETNARVVGGTEAGRNSWPSQISLQYRSGGSRYHTCGGTLIRQNWVMT
AAHCVDYQKTFRVVAGDHNLSQNDGTEQYVSVQKIVVHPYWNSDNVAAGYDIALLRLAQS
VTLNSYVQLGVLPQEGAILANNSPCYITGWGKTKTNGQLAQTLQQAYLPSVDYAICSSSS
YWGSTVKNTMVCAGGDGVRSGCQGDSGGPLHCLVNGKYSVHGVTSFVSSRGCNVSRKPTV
FTQVSAYISWINNVIASN
Drugs and Mode of Action
Drug(s) Alpha 1-PI Drug Info Approved Alpha-1 antitrypsin deficiency [1], [2]
Erdosteine Drug Info Approved Bronchitis [2]
Sivelestat Drug Info Phase 4 Discovery agent [3], [4]
Mdl 101,146 Drug Info Terminated Inflammatory disease [5]
PBI-1101 Drug Info Terminated Inflammatory disease [6]
SSR-69071 Drug Info Terminated Chronic obstructive pulmonary disease [7]
SYN-1134 Drug Info Terminated Cystic fibrosis [8]
WIN-63759 Drug Info Terminated Emphysema [9]
Inhibitor (2-BROMOETHYL)(2-'FORMYL-4'-AMINOPHENYL) ACETATE Drug Info [10]
(Tert-Butyloxycarbonyl)-Alanyl-Alanyl-Amine Drug Info [11]
Acetate Ion Drug Info [11]
Acetyl-Ala-Ala-Pro-Ala-trifluromethane Drug Info [12]
Acetyl-Pro-Ala-Pro-Ala-trifluoro methane Drug Info [12]
Alpha 1-PI Drug Info [13]
Dimethylformamide Drug Info [14]
GRASSYSTATIN A Drug Info [15]
Mdl 101,146 Drug Info [11]
MOLASSAMIDE Drug Info [16]
Para-Isopropylaniline Drug Info [11]
PBI-1101 Drug Info [17]
Sivelestat Drug Info [18]
SSR-69071 Drug Info [19]
SYN-1134 Drug Info [20]
Modulator Erdosteine Drug Info [2]
WIN-63759 Drug Info [21]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
References
REF 1Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003666)
REF 2Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 3ClinicalTrials.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 4(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 5Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007771)
REF 6Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018032)
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014569)
REF 8Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018646)
REF 9Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007449)
REF 10The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 11How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 12J 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 13Elastase inhibitors. J Soc Biol. 2001;195(2):143-50.
REF 14Liver disease associated with occupational exposure to the solvent dimethylformamide. Ann Intern Med. 1988 May;108(5):680-6.
REF 15J Med Chem. 2009 Sep 24;52(18):5732-47.Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
REF 16J Nat Prod. 2010 Mar 26;73(3):459-62.Molassamide, a depsipeptide serine protease inhibitor from the marine cyanobacterium Dichothrix utahensis.
REF 17CN patent application no. 1813706, Use of elastic protease inhibitor for preparing medicine for protecting cerebral hemorrhage.
REF 18Sivelestat (selective neutrophil elastase inhibitor) improves the mortality rate of sepsis associated with both ARDS and DIC patients. Shock. 2009 May 18.
REF 19Pivotal role for alpha1-antichymotrypsin in skin repair. J Biol Chem. 2011 Aug 19;286(33):28889-901.
REF 20EP patent application no. 1292314, Method for treating respiratory disorders associated with pulmonary elastic fiber injury comprising the use of glycosaminoglycans.
REF 21Biological activity of WIN 63759, an orally bioavailable inhibitor of human neutrophil elastase. Drug Development Research Volume 34, Issue 3, pages 306-316, March 1995.

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