Drug Metabolism in Drug Design and Development Basic Concepts and Practice

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