Nonsecosteroidal Ligands and Modulators of Vitamin D Receptor

Abstract A growing molecular and structural understanding of the vitamin D receptor (VDR) ligand-binding pocket and the need for new pharmacological agents targeting vitamin D-related disease states has led to the identification of several classes of nonsecosteroidal ligands. These ligands span a wide array of chemical diversity coupled with unique biochemical, cellular, and tissue-specific actions. While the number of described and characterized nonsecosteroidal chemical scaffolds remains small, they continue to hold promise in an ever-expanding number of human disease states where vitamin D physiology has demonstrable importance. This chapter is dedicated to describing the identification, physiochemical properties, functional behavior, and pharmacologic potential of nonsecosteroidal ligands that bind the VDR.