Hg5ln hpxr cell line

HG5LN were generated by transfection of cervical cancer HeLa cells with the (GAL4RE)5-betaGlobin-Luciferase-SV40-Neomycin plasmid.
HG5LN GAL4-hPXR cells were generated by transfection of HG5LN cells with the plasmid pSG5-GAL4-human PXR-puromycin.

The plasmid (GAL4RE)5-betaGlob-Luc-SVNeo contains a luciferase gene driven by a pentamer of yeast activator GAL4 binding sites in front of beta-globin promoter and a neomycin phosphotransferase gene under the control of SV40 promoter.
The pSG5-puro plasmid pSG5-human GAL4-hPXR-puromycin enables to express the DNA binding domain of the yeast activator GAL4 (GAL4 DBD) followed by the ligand binding domain of the human pregnane X receptor (hPXR LBD). Puromycin N-acetyl transferase selection marker expression confers resistance to puromycin.

Interest / Relevance: These cells enable to measure the hPXR (full and partial agonism, antagonism) of pharmaceuticals, environmental compounds
These cells enable to measure the hPXR activity of environmental (water, sediments), human (blood, urine adipose tissue) or food (water, vegetables, meat) samples.

SR12813 EC50 137 nM

Keywords: hPXR, luciferase, metabolism, clearance, colon and liver cancer, pharmaceutical and environmental chemicals

Scientist's name: Patrick BALAGUER
Patrick Balaguer

Publications:

Lemaire G, Benod C, Nahoum V, Pillon A, Boussioux AM, Guichou JF, Subra G, Pascussi JM, Bourguet W, Chavanieu A, Balaguer P. Discovery of a highly active ligand of human pregnane x receptor: a case study from pharmacophore modeling and virtual screening to in vivo biological activity. Mol Pharmacol. 2007 Sep,72(3):572-81.
Delfosse V, Dendele B, Huet T, Grimaldi M, Boulahtouf A, Gerbal-Chaloin S, Beucher B, Roecklin D, Muller C, Rahmani R, Cavaillès V, Daujat-Chavanieu M, Vivat V, Pascussi JM, Balaguer P*, Bourguet W. Synergistic activation of human pregnane X receptor by binary cocktails of pharmaceutical and environmental compounds. Nat Commun. 2015 Sep 3,6:8089.
Delfosse V, Granell M, Harrus D, Huet T, Bourguet M, Gardia-Parège C, Chiavarina B, Grimaldi M, Le Mével S, Gruszczyk J, Huang D, Blanc P, Demeneix B, Cianferani S, Fini JB, Balaguer P*, Bourguet W. Mechanistic insights into the synergistic activation of the RXR–PXR heterodimer by endocrine disruptor mixtures. PNAS 2021 Jan 5,118(1):e2020551118.

Reference:

RT00588

Type of research tool: Cell Lines

Therapy area(1): Oncology

Uses(1): Industry Research (screening, tox.studies, bioreactor, ...)

Inserm Transfert
Research Tools

E-mail

Rare disease: No

Last update: 28/08/2024

Hg5ln hpxr cell line

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