Mechanism of substrate transport and inhibition of the human LAT1-4F2hc amino acid transporter.
Journal
Cell discovery
ISSN: 2056-5968
Titre abrégé: Cell Discov
Pays: England
ID NLM: 101661034
Informations de publication
Date de publication:
23 Mar 2021
23 Mar 2021
Historique:
received:
16
11
2020
accepted:
30
01
2021
entrez:
24
3
2021
pubmed:
25
3
2021
medline:
25
3
2021
Statut:
epublish
Résumé
LAT1 (SLC7A5) is one of the representative light chain proteins of heteromeric amino acid transporters, forming a heterodimer with its heavy chain partner 4F2hc (SLC3A2). LAT1 is overexpressed in many types of tumors and mediates the transfer of drugs and hormones across the blood-brain barrier. Thus, LAT1 is considered as a drug target for cancer treatment and may be exploited for drug delivery into the brain. Here, we synthesized three potent inhibitors of human LAT1, which inhibit transport of leucine with IC
Identifiants
pubmed: 33758168
doi: 10.1038/s41421-021-00247-4
pii: 10.1038/s41421-021-00247-4
pmc: PMC7988154
doi:
Types de publication
Journal Article
Langues
eng
Pagination
16Subventions
Organisme : National Natural Science Foundation of China (National Science Foundation of China)
ID : 31971123
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