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The Sound of Evolution
Carfilzomib
Mechanism of action:
Carfilzomib is a second-generation proteasome inhibitor belonging to the epoxyketone peptide class. Carfilzomib binds to the beta5 subunit of the 26S proteasome and irreversibly inhibits its activity, leading to the accumulation of misfolded proteins that can no longer be degraded, thereby inducing endoplasmic reticulum stress and activating apoptotic pathways.
Reference(s):
1. Kortuem KM et al. (2013). Carfilzomib. Blood.
2. Kuhn DJ et al. (2007). Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. Blood.
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