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Biochem Biophys Res Commun. 1998 Apr 17;245(2):435-8.

Butein, a specific protein tyrosine kinase inhibitor.

Author information

1
Department of Experimental Surgery, Singapore General Hospital, Republic of Singapore. gesyeb@sgh.gov.sg

Abstract

Butein, a plant polyphenol, was shown to be a specific protein tyrosine kinase inhibitor. This compound inhibited not only the epidermal growth factor (EGF)-stimulated auto-phosphotyrosine level of EGF receptor in HepG2 cells but also tyrosine-specific protein kinase activities of EGF receptor (IC50 = 65 microM) and p60c-src (IC50 = 65 microM) in vitro. The inhibition was competitive to ATP and non-competitive to the phosphate acceptor, poly (Glu, Ala, Tyr) 6:3:1 for EGF receptor tyrosine kinase. In contrast, butein non-significantly inhibited the activities of serine- and threonine-specific protein kinases, such as protein kinase C (PKC) and cAMP-dependent protein kinase (PKA).

PMID:
9571170
DOI:
10.1006/bbrc.1998.8452
[Indexed for MEDLINE]

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