Figure 1: The effect of I281T mutation on CAR activity. (A) Activation of PBREM-driven reporter
by empty vector (white columns), wild-type CAR (black columns) or I281T mutant (grey
columns) full-length receptors. (B) Activation of GAL4-driven reporter by empty vector
(white), wild-type CAR (black) or I281T mutant (grey) LBD constructs. (C) Activation
of PBREM-driven reporter by empty vector (white), wild-type CAR (black) or I281T mutant
(grey) full-length receptors in the absence or presence of co-transfected coactivator
PGC1α. (D) Activation of PBREM-driven reporter wild-type CAR (black) or I281T mutant
(grey) full-length receptors after a 24-hour exposure to either vehicle DMSO, agonist
CITCO (1 μM) or inverse agonist S07662 (10 μM). The data shown in A - D are means
± SEM from three independent experiments, each with three biological replicates and
the results were normalized to the activity of wild-type CAR (set at 100). A and B
shows each independent experiment (Expt #1 - #3) while C and D show combined results.
* denotes a statistically significant difference (p < 0.017) to empty vector (A –
C) or wild-type CAR exposed to DMSO (D). # denotes a statistically significant difference
(p < 0.017) to wild-type CAR (A – D).
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