Ontology highlight
ABSTRACT:
SUBMITTER: Kawano S
PROVIDER: S-EPMC6572832 | biostudies-literature | 2019 Jun
REPOSITORIES: biostudies-literature
Kawano Satoshi S Ito Ken K Yahata Kenzo K Kira Kazunobu K Abe Takanori T Akagi Tsuyoshi T Asano Makoto M Iso Kentaro K Sato Yuki Y Matsuura Fumiyoshi F Ohashi Isao I Matsumoto Yasunobu Y Isomura Minetaka M Sasaki Takeo T Fukuyama Takashi T Miyashita Yusuke Y Kaburagi Yosuke Y Yokoi Akira A Asano Osamu O Owa Takashi T Kishi Yoshito Y
Scientific reports 20190617 1
Despite their outstanding antitumour activity in mice, the limited supply from the natural sources has prevented drug discovery/development based on intact halichondrins. We achieved a total synthesis of C52-halichondrin-B amine (E7130) on a >10 g scale with >99.8% purity under GMP conditions. Interestingly, E7130 not only is a novel microtubule dynamics inhibitor but can also increase intratumoural CD31-positive endothelial cells and reduce α-SMA-positive cancer-associated fibroblasts at pharma ...[more]