Proteasome inhibitors: new class of antitumor agents

  • Gordan Srkalović Cleveland Clinic Taussig Cancer Center, Myeloma Research Program
Keywords: proteasome inhibitors, antitumor agents

Abstract

The ubiquitin-proteasome pathway is the principal pathway for intracellular protein degradation1,2 (Fig 1). This pathway selectively degrades an extensive number of short-lived regulatory proteins involved in the control of normal cellular processes. In order to be degraded, proteins targeted by the ubiquitin-proteasome pathway are covalently tagged by polyubiquitination, via a three-step enzymatic process, which ultimately leads to their recognition and degradation, by the 26S proteasome in a highly specific and regulated manner. This process is accomplished by the sequential action of three enzymes: an ATP-dependent ubiquitin-activating enzyme (E1), an ubiquitin-conjugating enzyme (E2) and an ubiquitin-pro-tein ligase (E3).3 This cascade covalently links the C terminus of ubiquitin to a free amino group on the target protein, usually the ε-amino of a lysine residue.

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Proteasome inhibitors: new class of antitumor agents
Published
2003-11-20
How to Cite
1.
Srkalović G. Proteasome inhibitors: new class of antitumor agents. Bosn J of Basic Med Sci [Internet]. 2003Nov.20 [cited 2021Oct.18];3(4):5-10. Available from: https://www.bjbms.org/ojs/index.php/bjbms/article/view/3484
Section
Reviews