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Psoralenquinones as a Novel Class of Proteasome Inhibitors: Design, Synthesis and Biological Evaluation
Author(s) -
Marzaro Giovanni,
Gandin Valentina,
Marzano Christine,
Guiotto Adriano,
Chilin Adriana
Publication year - 2011
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201100041
Subject(s) - proteasome , protein subunit , class (philosophy) , computational biology , chemistry , biochemistry , biology , computer science , gene , artificial intelligence
Proteasome subunit specificity: Psoralenquinones were identified as a novel class of nonpeptide proteasome inhibitors. Depending on the scaffold decoration, these compounds demonstrate interesting subunit specificity. Interactions with Thr1, Thr21 and Ser129 are critical for inhibition.