Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis

Here we review our studies on the molecular design of nuclear receptor antagonists, including retinoic acid receptor (RAR) antagonists, retinoid X receptor (RXR) antagonists, androgen receptor (AR) antagonists, and vitamin D receptor (VDR) antagonists, based on inhibition of folding of helix 12, which contains a co-activator binding site. Recent progress in structural development studies of peroxisome proliferator-activated receptor (PPAR) ligands is also reviewed.

Here we review our studies on the molecular design of nuclear receptor antagonists, including RAR antagonists, RXR antagonists, AR antagonists, and VDR antagonists, based on inhibition of folding of helix 12, which contains a co-activator binding site.Figure optionsDownload as PowerPoint slide