Conservative mutageneic perturbations of amino acids connecting helix 12 in the 1alpha,25(OH)2-D3 receptor (VDR) to the ligand cause significant transactivational effects.

Abstract excerpt

The positioning of helix 12 activation domain of nuclear receptor proteins is critically important for gene regulation. Perturbations of the helix 12 by larger analogs may alter interactions with transcriptional machinery which might give rise to selectivity. To explore the topology of the ligand binding pocket and how the bound ligand conceivably gives rise to altered transcriptional efficiencies, we have...

Topics

Share this publication in a Topic to start or enrich a Post.

• Share to Amino Acids
• Share to Chlorocebus aethiops