(+)-Aeroplysinin-l: an Inhibitor of Intrinsic Protein Tyrosine Kinase Activity of EGF-Receptor-Kinase Complex

Autor: R. Steffen, Karin Pfeifer, M.-H. Kreuter, W. E. G. Müller, H. C. Schröder
Rok vydání: 1993
Předmět:
Zdroj: Cell and Tissue Culture Models in Dermatological Research ISBN: 9783642778193
DOI: 10.1007/978-3-642-77817-9_33
Popis: (+)-Aeroplysinin-l was isolated from the marine sponge Verongia aerophoba. It was found to inhibit the phosphorylation of lipocortin-like proteins mediated by a highly purified preparation of the epidermal growth factor (EGF) receptor-tyrosine protein kinase complex from MCF-7 breast carcinoma cells. (+)-Aeroplysinin-l blocked the EGF-dependent proliferation of both MCF-7 and ZR-75-1 human breast cancer cells and inhibited the ligand-induced endocytosis of the EGF receptor in vitro. Treatment with (+)-aeroplysinin-l in the concentration range of 0.25–0.5 μM resulted in a time- and dose-dependent total tumor cell death in vitro. From these data we conclude that (+)-aeroplysinin-l is a compound with strong anti-tumor effect on EGF-dependent tumor cell lines.
Databáze: OpenAIRE