Small-molecule inhibitor: carfilzomib

Summary

Name

Common name
carfilzomib
Other names
CFZ; Kyprolis; PR-171

Inhibition

History
Carfilzomib was described by Kuhn et al. (2007).
Peptidases inhibited
An irreversible inhibitor of the chymotrypsin-like activity of the proteasome and immunoproteasome.
Pharmaceutical relevance
Carfilzomib has been reported to be effective against several malignancies (see Literature).
DrugBank
620664

Chemistry

CID at PubChem
11556711
Structure
[carfilzomib (T01.010, T01.011, T01.012 inhibitor) structure ]
Chemical/biochemical name
(2S)-4-methyl-N-[(2S)-1-[[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]-2-[[(2S)-2-[(2-morpholin-4-ylacetyl)amino]-4-phenylbutanoyl]amino]pentanamide
Related inhibitors
Carfilzomib is structurally related to epoxomicin and PR-047 (Peese (2010)).