Development of Ligand-Drug Conjugates Targeting Melanoma through the Overexpressed Melanocortin 1 Receptor.
Journal
ACS pharmacology & translational science
ISSN: 2575-9108
Titre abrégé: ACS Pharmacol Transl Sci
Pays: United States
ID NLM: 101721411
Informations de publication
Date de publication:
09 Oct 2020
09 Oct 2020
Historique:
received:
23
06
2020
entrez:
19
10
2020
pubmed:
20
10
2020
medline:
20
10
2020
Statut:
epublish
Résumé
Melanoma is a lethal form of skin cancer. Despite recent breakthroughs of BRAF-V600E and PD-1 inhibitors showing remarkable clinical responses, melanoma can eventually survive these targeted therapies and become resistant. To solve the drug resistance issue, we designed and synthesized ligand-drug conjugates that couple cytotoxic drugs, which have a low cancer resistance issue, with the melanocortin 1 receptor (MC1R) agonist melanotan-II (MT-II), which provides specificity to MC1R-overexpressing melanoma. The drug-MT-II conjugates maintain strong binding interactions to MC1R and induce selective drug delivery to A375 melanoma cells through its MT-II moiety
Identifiants
pubmed: 33073191
doi: 10.1021/acsptsci.0c00072
pmc: PMC7551717
doi:
Types de publication
Journal Article
Langues
eng
Pagination
921-930Subventions
Organisme : NIDDK NIH HHS
ID : R01 DK017420
Pays : United States
Organisme : NIGMS NIH HHS
ID : R01 GM108040
Pays : United States
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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