121st General Meeting of the KCS

Type Symposium
Area Recent Trends in Drug Discovery
Room No. Room 302
Time THU 16:10-:
Code MEDI-2
Subject A Medicinal Chemistry Perspective for Targeting Nuclear Receptor Ligands for the Treatment of human diseases: Past, Present and Future
Authors Jungwook Chin
New Drug Development Center, DGMIF, Korea
Abstract Nuclear Receptors (NRs) work with other proteins that regulate the expression of specific proteins and regulate human development, homeostasis, and metabolism. Most of these regulatory genes are associated with a variety of diseases, which explain why about 13% of the US Food and Drug Administration (FDA) molecular targets have approved drugs that target nuclear receptors. Nuclear Receptors has recently come into the focus as a re-emerging drug target for the treatment of cancer and lipid associated diseases such as metabolic syndrome through a transcriptional regulation. At this symposium I will present the newly synthesized ligand of Nuclear Receptors and the development of an efficient synthetic pathway for these analogues. In addition, we evaluated the pharmacology in vitro, as well as its absorption, distribution, metabolism, excretion, and toxicity (ADMET). The results also show that ligands have a superior in vitro ADMET and in vivo pharmacokinetic (PK) profiles. Finally, I will talk about excluding Pan-Assay Interference Compounds (PAINS) compounds from the viewpoint of modern medicinal chemistry.
E-mail jwchin@dgmif.re.kr