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Hydroxyureas as Noncovalent Proteasome Inhibitors
Author(s) -
Gallastegui Nerea,
Beck Philipp,
Arciniega Marcelino,
Huber Robert,
Hillebrand Stefan,
Groll Michael
Publication year - 2012
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201106010
Subject(s) - proteasome , non covalent interactions , computational biology , chemistry , computer science , class (philosophy) , mechanism of action , biochemistry , combinatorial chemistry , pharmacology , medicine , biology , molecule , artificial intelligence , organic chemistry , hydrogen bond , in vitro
Inhibitors with a new mechanism of action are needed for 20S proteasome (CP) inhibition owing to the ineffectiveness of current market drugs against some types of solid tumors. A novel class of nonpeptidic CP inhibitors has been developed, which display reversible and noncovalent binding. The structure‐based design of these highly active and site‐specific inhibitors revealed unexplored binding subpockets.