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PDBsum entry 4lqi
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Hydrolase/hydrolase inhibitor
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PDB id
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4lqi
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Contents |
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250 a.a.
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244 a.a.
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241 a.a.
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242 a.a.
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233 a.a.
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244 a.a.
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243 a.a.
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222 a.a.
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204 a.a.
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198 a.a.
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212 a.a.
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222 a.a.
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233 a.a.
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196 a.a.
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References listed in PDB file
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Key reference
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Title
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Omuralide and vibralactone: differences in the proteasome- β-Lactone-γ-Lactam binding scaffold alter target preferences.
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Authors
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A.List,
E.Zeiler,
N.Gallastegui,
M.Rusch,
C.Hedberg,
S.A.Sieber,
M.Groll.
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Ref.
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Angew Chem Int Ed Engl, 2014,
53,
571-574.
[DOI no: ]
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PubMed id
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Abstract
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Despite their structural similarity, the natural products omuralide and
vibralactone have different biological targets. While omuralide blocks the
chymotryptic activity of the proteasome with an IC50 value of 47 nM,
vibralactone does not have any effect at this protease up to a concentration of
1 mM. Activity-based protein profiling in HeLa cells revealed that the major
targets of vibralactone are APT1 and APT2.
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