Production of human embryonic kidney 293T cells stably expressing C-X-C chemokine receptor type 4 (CXCR4) as a screening tool for anticancer lead compound targeting CXCR4.
Binding assay
CXCR4
Flow cytometry
HEK293T cells
Overexpression
Journal
Life sciences
ISSN: 1879-0631
Titre abrégé: Life Sci
Pays: Netherlands
ID NLM: 0375521
Informations de publication
Date de publication:
15 Aug 2022
15 Aug 2022
Historique:
received:
13
12
2021
revised:
19
05
2022
accepted:
23
05
2022
pubmed:
2
6
2022
medline:
18
6
2022
entrez:
1
6
2022
Statut:
ppublish
Résumé
The C-X-C chemokine-receptor type 4 (CXCR4) is an emerging target for cancer drug discovery due to its high expression in cancer cells. The present study aimed to produce CXCR4 overexpressing HEK293T cells for a non-radioactive binding assay as a platform to identify drug candidates targeting CXCR4. HEK293T cells stably expressing human CXCR4 were constructed by transfection of CXCR4 plasmids from the human CXCR4 gene. The CXCR4 overexpressing HEK293T cells were obtained by fluorescence-activated sorting and verified by conducting the competition binding assay of a known CXCR4 inhibitor, AMD3100 (plerixafor), to determine the IC The CXCR4 overexpressing HEK293T cells were produced with high expression (99.8%). The IC The verified non-radioactive binding assay can serve as an alternative screening tool for anticancer lead compounds targeting CXCR4 and an essential tool for proof of mechanism study in the drug discovery.
Identifiants
pubmed: 35643380
pii: S0024-3205(22)00361-7
doi: 10.1016/j.lfs.2022.120661
pii:
doi:
Substances chimiques
CXCR4 protein, human
0
Chemokine CXCL12
0
Cyclams
0
Heterocyclic Compounds
0
Receptors, CXCR4
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
120661Informations de copyright
Copyright © 2022 Elsevier Inc. All rights reserved.