Small-Molecule Gankyrin Inhibition as a Therapeutic Strategy for Breast and Lung Cancer.
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
14 07 2022
14 07 2022
Historique:
pubmed:
28
6
2022
medline:
16
7
2022
entrez:
27
6
2022
Statut:
ppublish
Résumé
Gankyrin is an oncoprotein responsible for the development of numerous cancer types. It regulates the expression levels of multiple tumor suppressor proteins (TSPs) in liver cancer; however, gankyrin's regulation of these TSPs in breast and lung cancers has not been thoroughly investigated. Additionally, no small-molecule gankyrin inhibitor has been developed which demonstrates potent anti-proliferative activity against gankyrin overexpressing breast and lung cancers. Herein, we are reporting the structure-based design of gankyrin-binding small molecules which potently inhibited the proliferation of gankyrin overexpressing A549 and MDA-MB-231 cancer cells, reduced colony formation, and inhibited the growth of 3D spheroids in an
Identifiants
pubmed: 35758870
doi: 10.1021/acs.jmedchem.2c00190
pmc: PMC9524259
mid: NIHMS1835462
doi:
Substances chimiques
Tumor Suppressor Proteins
0
Proteasome Endopeptidase Complex
EC 3.4.25.1
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
8975-8997Subventions
Organisme : NIGMS NIH HHS
ID : R15 GM126432
Pays : United States
Organisme : NIGMS NIH HHS
ID : SC2 GM139672
Pays : United States
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