Small-molecule inhibitor: salinosporamide A

Summary Structure Literature

Name

Common name: salinosporamide A
Other names: marizomib; NPI-0052

Inhibition

Peptidases inhibited: All three peptidase activities of the proteasome are inhibited (Macherla et al., 2005).
Mechanism: Inhibition is irreversible, resulting from covalent reactions analogous to those of clasto-lactacystin beta-lactone.
Pharmaceutical relevance: Salinosporamide A may be complementary to bortezomib in the treatment of multiple myeloma (Chauhan et al., 2005).

Chemistry

ChEBI: 48045
Structure
Formula weight: 314
Related inhibitors: salinosporamide B (the des-chloro analogue) and salinosporamide C (a decarboxylated pyrrole analogue) (Williams et al., 2005)