Methiothepin Increases Chemotherapy Efficacy against Resistant Melanoma Cells.
Antineoplastic Agents
/ pharmacology
Cell Line, Tumor
Cell Proliferation
/ drug effects
Doxorubicin
/ administration & dosage
Drug Resistance, Neoplasm
/ drug effects
Humans
Melanoma
/ drug therapy
Methiothepin
/ pharmacology
Patched-1 Receptor
/ metabolism
Pyridones
/ administration & dosage
Pyrimidinones
/ administration & dosage
Skin Neoplasms
/ drug therapy
Vemurafenib
/ administration & dosage
Ptch1
Ptch1 drug efflux inhibitor
chemotherapy resistance
melanoma
methiothepin
trametinib
vemurafenib
Journal
Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009
Informations de publication
Date de publication:
26 Mar 2021
26 Mar 2021
Historique:
received:
26
02
2021
revised:
16
03
2021
accepted:
23
03
2021
entrez:
3
4
2021
pubmed:
4
4
2021
medline:
25
5
2021
Statut:
epublish
Résumé
We previously reported that methiothepin, a small molecule known as a nonselective serotonin 5-HT receptor antagonist, inhibited the doxorubicin efflux activity of the Hedgehog receptor Ptch1 and enhanced the cytotoxic, pro-apoptotic, anti-proliferative, and anti-clonogenic effects of doxorubicin on adrenocortical carcinoma cells. Here, we show that methiothepin also inhibits doxorubicin efflux and increases doxorubicin cytotoxicity in melanoma cells which endogenously overexpress Ptch1. Melanoma patients having the BRAF
Identifiants
pubmed: 33810240
pii: molecules26071867
doi: 10.3390/molecules26071867
pmc: PMC8037503
pii:
doi:
Substances chimiques
Antineoplastic Agents
0
PTCH1 protein, human
0
Patched-1 Receptor
0
Pyridones
0
Pyrimidinones
0
Vemurafenib
207SMY3FQT
trametinib
33E86K87QN
Methiothepin
55D94103HL
Doxorubicin
80168379AG
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Subventions
Organisme : Agence Nationale de la Recherche
ID : ANR-15-IDEX-01
Organisme : Région PACA
ID : APRF program (2013-17362)
Organisme : Association France Cancer
ID : 2017-2020
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