title: Structural chemoproteomics and drug discovery.
abstract: Our laboratories have developed several technologies to accelerate drug discovery process on the basis of structural chemoproteomics. They include SPS technology for the efficient determination of protein structures, SCP technology for the rapid lead generation and SDF technology for the productive lead optimization. Using these technologies, we could determine many 3D structures of target proteins bound with biologically active chemicals including the structure of phosphodiesterase 5/Viagra complex and obtain highly potent compounds in animal models of obesity, diabetes, cancer and inflammation. In this paper, we will discuss concepts and applications of structural chemoproteomics for drug discovery.
authors.affiliation: CrystalGenomics, Inc., Asian Institute for Life Sciences, 388-1 Pungnap-dong, Songpa-gu, Seoul, 138-736, Korea.
authors.forename: Dongkyu
authors.initials: D
authors.lastname: Shin
authors.forename: Yong-Seok
authors.initials: YS
authors.lastname: Heo
authors.forename: Kyung Joo
authors.initials: KJ
authors.lastname: Lee
authors.forename: Cheol Min
authors.initials: CM
authors.lastname: Kim
authors.forename: Jung Min
authors.initials: JM
authors.lastname: Yoon
authors.forename: Jae Il
authors.initials: JI
authors.lastname: Lee
authors.forename: Young-Lan
authors.initials: YL
authors.lastname: Hyun
authors.forename: Young Ho
authors.initials: YH
authors.lastname: Jeon
authors.forename: Tae Gyu
authors.initials: TG
authors.lastname: Lee
authors.forename: Joong Myung
authors.initials: JM
authors.lastname: Cho
authors.forename: Seonggu
authors.initials: S
authors.lastname: Ro
mesh_terms: D000818:Animals; D001665:Binding Sites; D015195:Drug Design; D006801:Humans; D066298:In Vitro Techniques; D008958:Models, Molecular; D015394:Molecular Structure; D010726:Phosphodiesterase Inhibitors / Q000737:chemistry; D010727:Phosphoric Diester Hydrolases / Q000737:chemistry; D040901:Proteomics
chemical_list: D010726:Phosphodiesterase Inhibitors; D010727:Phosphoric Diester Hydrolases