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PDBsum entry 1hv7
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* Residue conservation analysis
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Enzyme class:
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E.C.3.4.21.36
- pancreatic elastase.
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Reaction:
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Hydrolysis of proteins, including elastin. Preferential cleavage: Ala-|-Xaa.
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DOI no:
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Bioorg Med Chem Lett
11:895-898
(2001)
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PubMed id:
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The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.
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S.J.Macdonald,
M.D.Dowle,
L.A.Harrison,
P.Shah,
M.R.Johnson,
G.G.Inglis,
G.D.Clarke,
R.A.Smith,
D.Humphreys,
C.R.Molloy,
A.Amour,
M.Dixon,
G.Murkitt,
R.E.Godward,
T.Padfield,
T.Skarzynski,
O.M.Singh,
K.A.Kumar,
G.Fleetwood,
S.T.Hodgson,
G.W.Hardy,
H.Finch.
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ABSTRACT
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The discovery of a potent intracellular inhibitor of human neutrophil elastase
which is orally active and has a long duration of action is described. The
pharmacodynamic and pharmacokinetic properties of a trans-lactam development
candidate, GW311616A, are described.
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Literature references that cite this PDB file's key reference
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PubMed id
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Reference
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V.Papayannopoulos,
K.D.Metzler,
A.Hakkim,
and
A.Zychlinsky
(2010).
Neutrophil elastase and myeloperoxidase regulate the formation of neutrophil extracellular traps.
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J Cell Biol,
191,
677-691.
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Y.Uchida,
M.C.Freitas,
D.Zhao,
R.W.Busuttil,
and
J.W.Kupiec-Weglinski
(2010).
The protective function of neutrophil elastase inhibitor in liver ischemia/reperfusion injury.
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Transplantation,
89,
1050-1056.
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Y.Uchida,
M.C.Freitas,
D.Zhao,
R.W.Busuttil,
and
J.W.Kupiec-Weglinski
(2009).
The inhibition of neutrophil elastase ameliorates mouse liver damage due to ischemia and reperfusion.
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Liver Transpl,
15,
939-947.
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J.C.Erve
(2006).
Chemical toxicology: reactive intermediates and their role in pharmacology and toxicology.
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Expert Opin Drug Metab Toxicol,
2,
923-946.
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V.Chung,
A.R.Carroll,
N.M.Gray,
N.R.Parry,
P.A.Thommes,
K.C.Viner,
and
E.A.D'Souza
(2005).
Development of cell-based assays for in vitro characterization of hepatitis C virus NS3/4A protease inhibitors.
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Antimicrob Agents Chemother,
49,
1381-1390.
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A.A.Lane,
and
T.J.Ley
(2003).
Neutrophil elastase cleaves PML-RARalpha and is important for the development of acute promyelocytic leukemia in mice.
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Cell,
115,
305-318.
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G.Müller
(2003).
Medicinal chemistry of target family-directed masterkeys.
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Drug Discov Today,
8,
681-691.
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H.Ohbayashi
(2002).
Neutrophil elastase inhibitors as treatment for COPD.
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Expert Opin Investig Drugs,
11,
965-980.
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S.Langston,
and
D.Barlocco
(2001).
Monitor: molecules and profiles.
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Drug Discov Today,
6,
962-964.
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The most recent references are shown first.
Citation data come partly from CiteXplore and partly
from an automated harvesting procedure. Note that this is likely to be
only a partial list as not all journals are covered by
either method. However, we are continually building up the citation data
so more and more references will be included with time.
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Links
