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The Core Structure of TMC‐95A Is a Promising Lead for Reversible Proteasome Inhibition
Author(s) -
Kaiser Markus,
Groll Michael,
Renner Christian,
Huber Robert,
Moroder Luis
Publication year - 2002
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 - 10.1002/1521-3773(20020301)41:5<780::aid-anie780>3.0.co;2-v
Subject(s) - proteasome , core (optical fiber) , chemistry , work (physics) , lead (geology) , biophysics , biochemistry , materials science , biology , physics , paleontology , composite material , thermodynamics
Based on information from the X‐ray structure of the TMC‐95A/proteasome complex, TMC‐95A ( A ) was reduced to the minimum core structure ( B ). The inhibitory potency of the synthetic analogue confirms that the simplified ring structure may well serve as the lead for further improvement of affinity and selectivity of reversible proteasome inhibitors.