3',4'-Dihydroxyl Groups in Luteolin are Important for Its Inhibitory Activities against ADAMTS-4

Autor: Jiwon Choi, Yangmee Kim, Jin-Kyoung Kim, Ki-Woong Jeong, Byung-Ha Chang, Jee-Young Lee
Rok vydání: 2012
Předmět:
Zdroj: Bulletin of the Korean Chemical Society. 33:2907-2909
ISSN: 0253-2964
DOI: 10.5012/bkcs.2012.33.9.2907
Popis: A disintegrin and metalloprotease with thrombospondin domains (ADAMTS) are a member of peptidase and involved in processing of von Willebrand factor as well as cleavage of aggrecan, versican, brevican and neurocan. Among 19 subfamilies of human ADAMTS, ADAMTS-4 is a zinc-binding metalloprotease and is a famous therapeutic target for arthritis. It has been reported that a flavonoid luteolin shows inhibitory activity against ADMATS-4. In this study, we verified that luteolin is a potent inhibitor of ADAMTS-4 and probed the molecular basis of its action. On the basis of a docking study, we proposed a binding model between luteolin and ADAMTS-4 in which 3',4'-dihydroxyl groups in luteolin formed hydrogen bonding with ADMATS-4 and these interactions are important for its inhibitory activity against ADAMTS-4.
Databáze: OpenAIRE