Use of Cryopreserved Transiently Transfected Cells in High-Throughput Pregnane X Receptor Transactivation Assay-Reference-Cited by-同舟云学术

Use of Cryopreserved Transiently Transfected Cells in High-Throughput Pregnane X Receptor Transactivation Assay

Published:2007-01-11 Issue:2 Volume:12 Page:248-254
ISSN:1087-0571
Container-title:Journal of Biomolecular Screening
language:en
Short-container-title:J Biomol Screen

Author:

Zhu Zhengrong,Puglisi Jaime,Connors David,Stewart Jeremy,Herbst John¹,Marino Anthony²,Sinz Michael,O'Connell Jonathan,Banks Martyn,Dickinson Kenneth,Cacace Angela¹

Affiliation:

1. Bristol-Myers Squibb Company, Wallingford, Connecticut, New Jersey

2. Bristol-Myers Squibb Company, Lawrenceville, New Jersey

Abstract

Cryopreserved, transiently transfected HepG2 cells were compared to freshly transfected HepG2 cells for use in a pregnane X receptor (PXR) transactivation assay. Assay performance was similar for both cell preparations; however, cryopreserved cells demonstrated less interassay variation. Validation with drugs of different PXR activation potencies and efficacies demonstrated an excellent correlation ( r2 > 0.95) between cryopreserved and fresh cells. Cryopreservation did not change the effect of known CYP3A4 inducers that have poor cell permeability, indicating that cryopreservation had little effect on membrane permeability. In addition, cryopreserved HepG2 cells did not exhibit enhanced susceptibility to cytotoxic compounds compared to transiently transfected control cells. The use of cryopreserved cells enables this assay to run with enhanced efficiency.

Publisher

Elsevier BV

Link

http://journals.sagepub.com/doi/pdf/10.1177/1087057106297828

Reference35 articles.

1. Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction

2. The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions.

3. Correlation of High-Throughput Pregnane X Receptor (PXR) Transactivation and Binding Assays

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