Relationship between flavonoid structure and inhibition of farnesyl protein transferase.
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.
Kang
Hyun-Mi
HM
Korea Research Institute of Bioscience and Biotechnology, P.O. Box 115, Yusung, Taejon 305-600, Republic of Korea.
Kim
Jong-Han
JH
Lee
Mi-Young
MY
Son
Kwang-Hee
KH
Yang
Deok Cho
DC
Baek
Nam-In
NI
Kwon
Byoung-Mog
BM
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
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