Antitumor activity of erbstatin, a tyrosine protein kinase inhibitor.

Abstract

A tyrosine protein kinase inhibitor, erbstatin, showed no antineoplastic effect on L-1210 mouse leukemia when it was injected alone. Erbstatin was found to be inactivated by incubation in serum, but not in dialyzed serum. It was also inactivated in reconstituted serum containing dialyzed serum components and ferric or ferrous ion. Because erbstatin was considered to be inactivated by the ferric or ferrous ion in serum, foroxymithine, which is a potent chelator for the ferric ion, was given to the mice together with erbstatin. Administration of both erbstatin and foroxymithine showed antineoplastic activity against L-1210 leukemia.

• Authors: M Imoto, K Umezawa, K Komuro, T Sawa, T Takeuchi, H Umezawa
• Journal: Japanese journal of cancer research : Gann (Jpn J Cancer Res) Vol. 78 Issue 4 Pg. 329-32 (Apr 1987) ISSN: 0910-5050 [Print] Japan
• PMID: 3108212 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• DNA, Neoplasm
• Hydroquinones
• Neoplasm Proteins
• Peptides
• RNA, Neoplasm
• foroxymithine
• Protein-Tyrosine Kinases
• erbstatin

Topics

• Animals
• DNA, Neoplasm (biosynthesis)
• Hydroquinones (metabolism, pharmacology, therapeutic use)
• Leukemia L1210 (drug therapy)
• Metabolic Clearance Rate (drug effects)
• Mice
• Neoplasm Proteins (biosynthesis)
• Peptides (pharmacology)
• Protein-Tyrosine Kinases (antagonists & inhibitors)
• RNA, Neoplasm (biosynthesis)