Insulin-Degrading Enzyme Is a Non Proteasomal Target of Carfilzomib and Affects the 20S Proteasome Inhibition by the Drug.
cancer
carfilzomib
insulin-degrading enzyme
neurodegeneration
proteasome
Journal
Biomolecules
ISSN: 2218-273X
Titre abrégé: Biomolecules
Pays: Switzerland
ID NLM: 101596414
Informations de publication
Date de publication:
16 02 2022
16 02 2022
Historique:
received:
10
08
2021
revised:
12
01
2022
accepted:
27
01
2022
entrez:
25
2
2022
pubmed:
26
2
2022
medline:
9
4
2022
Statut:
epublish
Résumé
Carfilzomib is a last generation proteasome inhibitor (PI) with proven clinical efficacy in the treatment of relapsed/refractory multiple myeloma. This drug is considered to be extremely specific in inhibiting the chymotrypsin-like activity of the 20S proteasome, encoded by the β5 subunit, overcoming some bortezomib limitations, the first PI approved for multiple myeloma therapy which is however burdened by a significant toxicity profile, due also to its off-target effects. Here, molecular approaches coupled with molecular docking studies have been used to unveil that the Insulin-Degrading Enzyme, a ubiquitous and highly conserved Zn
Identifiants
pubmed: 35204815
pii: biom12020315
doi: 10.3390/biom12020315
pmc: PMC8869475
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
Oligopeptides
0
Pharmaceutical Preparations
0
Proteasome Inhibitors
0
carfilzomib
72X6E3J5AR
Insulysin
EC 3.4.24.56
Proteasome Endopeptidase Complex
EC 3.4.25.1
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
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