Soloxolone
ABC transporters
P-glycoprotein
cancer
chemotherapy
multidrug resistance
pentacyclic triterpenoids
soloxolone
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
18 Oct 2024
18 Oct 2024
Historique:
received:
17
09
2024
revised:
15
10
2024
accepted:
16
10
2024
medline:
26
10
2024
pubmed:
26
10
2024
entrez:
26
10
2024
Statut:
epublish
Résumé
Multidrug resistance (MDR) remains a significant challenge in cancer therapy, primarily due to the overexpression of transmembrane drug transporters, with P-glycoprotein (P-gp) being a central focus. Consequently, the development of P-gp inhibitors has emerged as a promising strategy to combat MDR. Given the P-gp targeting potential of soloxolone amides previously predicted by us by an absorption, distribution, metabolism, excretion, and toxicity (ADMET) analysis, the aim of the current study was to experimentally verify their P-gp inhibitory and MDR reversing activities in vitro. Screening of soloxolone amides as modulators of P-gp using molecular docking and cellular P-gp substrate efflux assays revealed the ability of compound
Identifiants
pubmed: 39459307
pii: molecules29204939
doi: 10.3390/molecules29204939
pii:
doi:
Substances chimiques
ATP Binding Cassette Transporter, Subfamily B, Member 1
0
Antineoplastic Agents
0
Doxorubicin
80168379AG
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Russian Science Foundation
ID : 23-14-00374
Organisme : Russian state-funded budget project of ICBFM SB RAS
ID : 121031300044-5