title: The first naturally occurring Tie2 kinase inhibitor.
abstract: [structure: see text] Bioassay-guided fractionation of the plant Acacia aulacocarpa, guided by a bioassay for Tie2 tyrosine kinase activity, yielded the novel triterpene 3,21-dioxo-olean-18-en-oic acid (1) as the first naturally occurring non-protein inhibitor of Tie2 kinase. The structure of 1 was assigned by analysis of spectral data. In addition to its activity as an inhibitor of Tie2 kinase, compound 1 also shows modest activity against a variety of cultured mammalian cells.
authors.affiliation: Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, Virginia 24061, USA.
authors.forename: B N
authors.initials: BN
authors.lastname: Zhou
authors.forename: R K
authors.initials: RK
authors.lastname: Johnson
authors.forename: M R
authors.initials: MR
authors.lastname: Mattern
authors.forename: P W
authors.initials: PW
authors.lastname: Fisher
authors.forename: D G
authors.initials: DG
authors.lastname: Kingston
mesh_terms: D000045:Acacia / Q000737:chemistry*; D000818:Animals; D002478:Cells, Cultured; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D015394:Molecular Structure; D009828:Oleanolic Acid / Q000031:analogs & derivatives / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D010936:Plant Extracts / Q000737:chemistry*; D020794:Receptor Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D042787:Receptor, TIE-2; D014315:Triterpenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology
chemical_list: C447982:3,21-dioxo-olean-18-en-oic acid; D004791:Enzyme Inhibitors; D010936:Plant Extracts; D014315:Triterpenes; D009828:Oleanolic Acid; D020794:Receptor Protein-Tyrosine Kinases; D042787:Receptor, TIE-2