. Author manuscript; available in PMC: 2017 Mar 15.

Published in final edited form as: Biochem Pharmacol. 2016 Feb 18;104:131–138. doi: 10.1016/j.bcp.2016.02.009

Table 1.

Summary of activity of hPXR WT and mutants in HepG2 cells (CYP3A4 promoter activity; see Figures 1, 2A and 4 for details).

Type of substituting residue(s)	WT hPXR or hPXR mutants	RIF activity	SR activity	TO activity
None	hPXR	+++	+++	+++
Hydrophobic	W299A	+++	+++	+
Hydrophobic	W299V	+++	not tested	not tested
Charged	W299D	+/−	+/−	+/−
	W299E	+/−	+/−	+/−
	W299K	+/−	+/−	+/−
Double mutants	W299A-F288A	+++	+/−	+/−
Double mutants	W299D-F288A	+/−	+/−	+/−
Triple mutant	W299A-F288A-Y306A	−	−	−

+++ strongly active;

+ weakly active;

+/− very weak or inactive;

− complete loss of function