Kaiser, Markus; Groll, Michael; Renner, Christian; Huber, Robert; Moroder, Luis:
The Core Structure of TMC-95A Is a Promising Lead for Reversible Proteasome Inhibition
2002
In: Angewandte Chemie - International Edition, Jg. 41 (2002), Heft 5, S. 780 - 783
Artikel/Aufsatz in Zeitschrift2002Biologie
Titel:
The Core Structure of TMC-95A Is a Promising Lead for Reversible Proteasome Inhibition
Autor(in):
Kaiser, MarkusLSF; Groll, Michael; Renner, Christian; Huber, RobertLSF; Moroder, Luis
Erscheinungsjahr
2002
WWW URL

Abstract:

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.