title: Design and synthesis of highly potent fumagillin analogues from homology modeling for a human MetAP-2.
abstract: New fumagillin analogues were designed through structure-based molecular modeling with a human methionine aminopeptidase-2. Among the fumagillin analogues, cinnamic acid ester derivative CKD-731 showed 1000-fold more potent proliferation inhibitory activity on endothelial cell than TNP-470.
authors.affiliation: Chong Kun Dang Research Institute, Chungcheongnamdo, South Korea.
authors.forename: C K
authors.initials: CK
authors.lastname: Han
authors.forename: S K
authors.initials: SK
authors.lastname: Ahn
authors.forename: N S
authors.initials: NS
authors.lastname: Choi
authors.forename: R K
authors.initials: RK
authors.lastname: Hong
authors.forename: S K
authors.initials: SK
authors.lastname: Moon
authors.forename: H S
authors.initials: HS
authors.lastname: Chun
authors.forename: S J
authors.initials: SJ
authors.lastname: Lee
authors.forename: J W
authors.initials: JW
authors.lastname: Kim
authors.forename: C I
authors.initials: CI
authors.lastname: Hong
authors.forename: D
authors.initials: D
authors.lastname: Kim
authors.forename: J H
authors.initials: JH
authors.lastname: Yoon
authors.forename: K T
authors.initials: KT
authors.lastname: No
mesh_terms: D000595:Amino Acid Sequence; D000626:Aminopeptidases / Q000737:chemistry*; D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D002417:Cattle; D002460:Cell Line; D002934:Cinnamates / Q000138:chemical synthesis / Q000494:pharmacology; D003510:Cyclohexanes; D015195:Drug Design; D004852:Epoxy Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D005231:Fatty Acids, Unsaturated / Q000138:chemical synthesis* / Q000494:pharmacology*; D006131:Growth Inhibitors / Q000494:pharmacology; D006801:Humans; D007941:Leukemia P388 / Q000473:pathology; D008666:Metalloendopeptidases / Q000737:chemistry*; D051379:Mice; D008958:Models, Molecular; D008969:Molecular Sequence Data; D017386:Sequence Homology, Amino Acid; D012717:Sesquiterpenes; D013329:Structure-Activity Relationship
chemical_list: D020533:Angiogenesis Inhibitors; D002934:Cinnamates; D003510:Cyclohexanes; D004852:Epoxy Compounds; D005231:Fatty Acids, Unsaturated; D006131:Growth Inhibitors; D012717:Sesquiterpenes; C404215:CKD 731; C026211:fumagillin; D000626:Aminopeptidases; C106541:methionine aminopeptidase 2; D008666:Metalloendopeptidases