Words similar to cis-
Example sentences for: cis-
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Purified CAR and RXR proteins were produced in bacteria and preincubated overnight at 4°C alone or in combination, and in the presence or absence of 10 -5M androstanol, 10 -6M TCPOBOP, 10 -6M of 9 cis-RA, as appropriate.
The effects of specific RXR ligands on the CAR/RXR heterodimer have not been characterized, although high concentrations of both 9-cis-RA and all-trans retinoic acid have been reported to block PB induction of the CAR targets CYP2B1 and CYP2B2 in primary rat hepatocytes [ 17 ] . In addition, a recent report suggests that both compounds decrease TCPOBOP-dependent CAR transactivation [ 18 ] . In both cases, these effects were primarily attributed to sequestration of limiting amounts of RXR into ligand-dependent homodimers or heterodimers with other receptors.
As expected, 9-cis-RA stimulated coactivator binding to RXR alone, and the basal interaction of CAR with SRC-3 was enhanced by TCPOBOP and decreased by androstanol (Fig.
Initial functional results suggested that transactivation by CAR/RXR heterodimers is not affected by RXR ligands, including 9-cis-RA or synthetic rexinoids, indicating that CAR is a non-permissive RXR partner.
In addition, SRC-3 binding to the heterodimer was decreased by androstanol and this effect was largely blocked by 9-cis-RA.