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PDBsum entry 5m2b
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Hydrolase/hydrolase inhibitor
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PDB id
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5m2b
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Contents |
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250 a.a.
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244 a.a.
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240 a.a.
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235 a.a.
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231 a.a.
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243 a.a.
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241 a.a.
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226 a.a.
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204 a.a.
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195 a.a.
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211 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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Structural elucidation of a nonpeptidic inhibitor specific for the human immunoproteasome.
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Authors
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H.Cui,
R.Baur,
C.Le chapelain,
C.Dubiella,
W.Heinemeyer,
E.M.Huber,
M.Groll.
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Ref.
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Chembiochem, 2017,
18,
523-526.
[DOI no: ]
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PubMed id
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Abstract
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Selective inhibition of the immunoproteasome is a promising approach towards the
development of immunomodulatory drugs. Recently, a class of substituted thiazole
compounds that combine a nonpeptidic scaffold with the absence of an
electrophile was reported in a patent. Here, we investigated the mode of action
of the lead compound by using a sophisticated chimeric yeast model of the human
immunoproteasome for structural studies. The inhibitor adopts a unique
orientation perpendicular to the β5i substrate-binding channel. Distinct
interactions between the inhibitor and the subpockets of the human
immunoproteasome account for its isotype selectivity.
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