Small-molecule inhibitor: PR-047
Inhibition
- History
- The design and synthesis of PR-047 were described by Zhou et al. (2009).
- Peptidases inhibited
- Chymotrypsin-like activities of the proteasome and immunoproteasome, with Ki values of 55 and 66 nM, respectively (Zhou et al. , 2009).
- Mechanism
- Inhibition is irreversible, following covalent reaction of the inhibitor with the active site of the peptidase.
- Pharmaceutical relevance
- In vivo anti-tumour activity has been demonstrated by Zhou et al. (2009).
- DrugBank
- 620530
Chemistry
- CID at PubChem
- 44591654
- Structure
![[PR-047 (T01.012, T01.015 inhibitor) structure ]](http://pubchem.ncbi.nlm.nih.gov/image/imgsrv.fcgi?t=l&cid=44591654)
- Chemical/biochemical name
- 2-Me-5-thiazole-Ser(OMe)-Ser(OMe)-Phe-ketoepoxide
- Related inhibitors
- PR-047 is structurally related to epoxomicin and carfilzomib, which are also epoxyketone inhibitors of the proteasome.
