[PPARgamma targeted genome-based drug discovery; present and future direction].
ABSTRACT Peroxisome proliferator-activated receptor gamma (PPARgamma) is known to regulate growth arrest and terminal differentiation of adipocytes initially, and glitazones are used as a new class of antidiabetic drugs clinically. Recent understanding of the functions of PPARs, using genome-wide analysis, as pleiotropic regulators of biological responses, including not only lipid, lipoprotein, glucose homeostasis, but also inflammation, differentiation and proliferation of various cancer cells, and memory, have provided an opportunity to develop novel PPARs ligands with characteristic subtype selectivity. Such ligands are not only chemical tools to investigate the functions of PPARs, but also candidates for the treatment of PPARs-mediated diseases. This article summarizes recent topics of the medicinal chemistry work on the design, synthesis and pharmacological evaluation of PPARs related agents.