Preferential targeting of MCL-1 by a hydrocarbon-stapled BIM BH3 peptide.
BH3 mimetic
BIM
MCL-1
apoptosis
stapled peptides
Journal
Oncotarget
ISSN: 1949-2553
Titre abrégé: Oncotarget
Pays: United States
ID NLM: 101532965
Informations de publication
Date de publication:
22 Oct 2019
22 Oct 2019
Historique:
received:
08
02
2019
accepted:
04
10
2019
entrez:
7
11
2019
pubmed:
7
11
2019
medline:
7
11
2019
Statut:
epublish
Résumé
BCL-2 family proteins are central regulators of apoptosis and represent prime therapeutic targets for overcoming cell death resistance in malignancies. However, plasticity of anti-apoptotic members, such as MCL-1, often allows for a switch in cell death dependency patterns that lie outside the binding profile of targeted BH3-mimetics. Therefore discovery of therapeutics that effectively inactivate all anti-apoptotic members is a high priority. To address this we tested the potency of a hydrocarbon stapled BIM BH3 peptide (BIM SAHB
Identifiants
pubmed: 31692812
doi: 10.18632/oncotarget.27262
pii: 27262
pmc: PMC6817437
doi:
Types de publication
Journal Article
Langues
eng
Pagination
6219-6233Subventions
Organisme : NCI NIH HHS
ID : F30 CA221250
Pays : United States
Organisme : NCI NIH HHS
ID : K08 CA151450
Pays : United States
Déclaration de conflit d'intérêts
CONFLICTS OF INTEREST The authors report no conflicts of interest.
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