Drug Metabolism in Drug Design and Development Basic Concepts and Practice

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TABLE 17.2 Summary of Human PXR reporter gene assays used in several laboratories.Author


PXR Construct

Reporter gene construct

Cell line

Maximal induction

References

Bertilsson et al

GAL

4–LBD

4USA-Luciferase

Caco-2



15-fold

Bertilsson et al., (1998)

pCMV

–PXR

CYP3A4(ER)6-Luciferase

Caco-2



5-fold

Blumberg et al

GAL

–LBD

Tk-USA-Luciferase

CV-1



12-fold

Blumberg et al., (1998)

pSG

5–PXR

Tk-(ER)6-Luciferase

CV-1



12-fold

Lehmann et al

pSG

5–PXR

(ER)6-tk-CAT

CV-1



9-fold

Lehmann et al., (1998)

Goodwin et al

pSG

5–PXR

CYP3A4(



7836 to 208)



(

362 to 53)-Luciferase

HepG2



40-fold

Goodwin et al., (1999)

El-Sankary et al

pSG

5–PXR

CYP3A4(



1087 to



57)-SPAP

HepG2



3-fold

El-Sankary et al., (2000)

561
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