Proteasome inhibition in human breast cancer cells with high catechol-O-methyltransferase activity by green tea polyphenol EGCG analogs.
A pro-drug 8 of a synthetic analog 7 is more active in its antiproliferative activity against human breast cancer MDA-MB-231 cells possessing high catechol-O-methyltransferase (COMT) activity than the pro-drugs of EGCG and the analog 5. The higher activity of 8 is attributed to it not being a substrate of COMT.
Huo
Congde
C
Department of Chemistry, McGill University, Montreal, Quebec, Canada.
Yang
Huanjie
H
Cui
Qiuzhi Cindy
QC
Dou
Q Ping
QP
Chan
Tak Hang
TH
D000972:Antineoplastic Agents, Phytogenic / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000201:enzymology; D002392:Catechin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002394:Catechol O-Methyltransferase / Q000378:metabolism*; D002470:Cell Survival / Q000187:drug effects; D005260:Female; D006801:Humans; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D046988:Proteasome Endopeptidase Complex / Q000378:metabolism; D061988:Proteasome Inhibitors; D013662:Tea / Q000737:chemistry*
D000972:Antineoplastic Agents, Phytogenic; D011355:Prodrugs; D061988:Proteasome Inhibitors; D013662:Tea; D002392:Catechin; C045651:epigallocatechin gallate; D002394:Catechol O-Methyltransferase; D046988:Proteasome Endopeptidase Complex; C061553:ATP dependent 26S protease