The Core Structure of TMC-95A Is a Promising Lead for Reversible Proteasome Inhibition
In: Angewandte Chemie - International Edition, Jg. 41 (2002) ; Nr. 5, S. 780–783
ISSN: 0044-8249, 0570-0833, 1433-7851
Zeitschriftenaufsatz / Fach: Biologie
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.