title: Relationship between flavonoid structure and inhibition of farnesyl protein transferase.
abstract: Flavonoids are well-known phytochemicals that are produced by various plants in high quantities. The chemopreventive activity of flavonoids is dependent on their structural features. The studies of structure-FPTase inhibitory activity indicated that the number, position and substitution of hydroxyl groups of the A and B rings of flavonoid, and unsaturation of the C2-C3 bond are important factors affecting inhibition on FPTase by flavonoids. A couple of flavonoids inhibited FPTase and also the growth of human tumor cell lines, especially butein, which strongly inhibited the growth of colon cancer cell line (HCT116). However, flavanones and flavanols did not inhibit FPTase nor the growth of tumor cells.
authors.affiliation: Korea Research Institute of Bioscience and Biotechnology, P.O. Box 115, Yusung, Taejon 305-600, Republic of Korea.
authors.forename: Hyun-Mi
authors.initials: HM
authors.lastname: Kang
authors.forename: Jong-Han
authors.initials: JH
authors.lastname: Kim
authors.forename: Mi-Young
authors.initials: MY
authors.lastname: Lee
authors.forename: Kwang-Hee
authors.initials: KH
authors.lastname: Son
authors.forename: Deok Cho
authors.initials: DC
authors.lastname: Yang
authors.forename: Nam-In
authors.initials: NI
authors.lastname: Baek
authors.forename: Byoung-Mog
authors.initials: BM
authors.lastname: Kwon
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D063065:Organophosphonates / Q000737:chemistry / Q000494:pharmacology*; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D010946:Plants, Medicinal
chemical_list: C436083:2-(2-oxo-2-((3,7,11-trimethyl-2,6,10-dodecatrienyl)oxy)aminoethyl)phosphonic acid, (2,2-dimethyl-1-oxopropoxy)methyl ester sodium; D000972:Antineoplastic Agents, Phytogenic; D005419:Flavonoids; D063065:Organophosphonates; D010936:Plant Extracts; D019883:Alkyl and Aryl Transferases; C064911:p21(ras) farnesyl-protein transferase