Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.
A novel class of phenylpyrazole fused Wieland-Miescher ketone derivatives are high affinity, receptor specific, selective modulators of glucocorticoid receptor (GR) mediated transcription in vitro, dissociating transactivation, AP-1 repression, and NF-kappaB repression from each other.
Shah
Nilesh
N
Graduate Group in Biophysics, University of California--San Francisco, San Francisco, CA 94143-2280, USA.
Scanlan
Thomas S
TS
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001667:Binding, Competitive; D002460:Cell Line; D005454:Fluorescence Polarization; D006801:Humans; D066298:In Vitro Techniques; D007659:Ketones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008024:Ligands; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011965:Receptors, Glucocorticoid / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D007659:Ketones; D008024:Ligands; D011720:Pyrazoles; D011965:Receptors, Glucocorticoid