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TitleStructural Insights into Salinosporamide a Mediated Inhibition of the Human 20S Proteasome.
Journal, issue, pagesMolecules, Vol. 30, Issue 6, Year 2025
Publish dateMar 20, 2025
AuthorsHagen Sülzen / Pavla Fajtova / Anthony J O'Donoghue / Jan Silhan / Evzen Boura /
PubMed AbstractThe 20S proteasome, a critical component of the ubiquitin-proteasome system, plays a central role in regulating protein degradation in eukaryotic cells. Marizomib (MZB), also known as salinosporamide ...The 20S proteasome, a critical component of the ubiquitin-proteasome system, plays a central role in regulating protein degradation in eukaryotic cells. Marizomib (MZB), also known as salinosporamide A, is a natural γ-lactam-β-lactone compound derived from and is a potent 20S proteasome covalent inhibitor with demonstrated anticancer properties. Its broad-spectrum inhibition of all three proteasome subunits and its ability to cross the blood-brain barrier has made it a promising therapeutic candidate for glioblastoma. In addition to this, MZB also demonstrates significant inhibition against the 20S proteasome of (20S), a protozoan parasite, suggesting its potential for parasitic treatments. Here, we present the cryo-EM structure of the human 20S proteasome in complex with MZB at 2.55 Å resolution. This structure reveals the binding mode of MZB to all six catalytic subunits within the two β-rings of the 20S proteasome, providing a detailed molecular understanding of its irreversible inhibitory mechanism. These findings enhance the therapeutic potential of MZB for both cancer and parasitic diseases at the molecular level and highlight marine-derived natural products in targeting the proteasome for therapeutic applications.
External linksMolecules / PubMed:40142161 / PubMed Central
MethodsEM (single particle)
Resolution2.55 Å
Structure data

52296

9hmn

EMDB-52296, PDB-9hmn:
CryoEM structure of human 20S proteasome in complex with proteasome inhibitor Salinosporamid A
Method: EM (single particle) / Resolution: 2.55 Å

Chemicals

ChemComp-SA1:
(3AR,6R,6AS)-6-((S)-((S)-CYCLOHEX-2-ENYL)(HYDROXY)METHYL)-6A-METHYL-4-OXO-HEXAHYDRO-2H-FURO[3,2-C]PYRROLE-6-CARBALDEHYDE / anticancer, inhibitor*YM

Source
  • homo sapiens (human)
KeywordsHYDROLASE / Inhibitor / 20S proteasome / Salinosporamid A

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