[A new therapy with bortezomib, an oncologic medicinal product of the year 2004].

Proteasome-mediated proteolysis is a mechanism for mediating important regulatory proteins within the cell. Proteins that have been targeted for degradation by the proteasome are convalently tagged with a poly-ubiquitin protein chain prior to be recognized by the 19S subunit of proteasome. This degradation system controls the expression of a wide variety of cellular targets including tumor suppressors such as p53, inhibitor of nuclear factor NFkappaB, cyclin-dependent kinase inhibitors such as p21 and p27.

[Glucuronyl paclitaxel (Taxol) derivatives as tumor activated prodrugs].

Three glucuronyl prodrugs of paclitaxel have been synthesized in order to be activated by the B-glucuronidase present within the necrotic areas of tumors. As three compartments containing prodrugs, they include a specifier, a self immolative spacer and the drug. In vitro testing clearly indicates that the two former prodrugs are stable and are more or less detoxified.