J Nat Prod. 1989 Nov-Dec;52(6):1252-7.

Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus.

Onoda T, Iinuma H, Sasaki Y, Hamada M, Isshiki K, Naganawa H, Takeuchi T, Tatsuta K, Umezawa K.

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Institute of Microbial Chemistry, Tokyo, Japan.

Abstract

A potent tyrosine kinase inhibitor, lavendustin A [1], has been isolated from a butyl acetate extract of Streptomyces griseolavendus culture filtrate. It inhibits epidermal growth factor receptor-associated tyrosine kinase with an IC50 of 4.4 ng/ml, which is about 50 times more inhibitory than erbstatin. It does not inhibit protein kinase A or C. Its structure, determined by spectral data and total synthesis, is novel, having a tertiary amine in the center with substituted benzyl and phenyl groups. Lavendustin A competes with ATP and is noncompetitive with the peptide. Its structure-activity relationship is discussed.

PMID:: 2614420; [PubMed - indexed for MEDLINE]

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Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces...
Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus.
J Nat Prod. 1989 Nov-Dec ;52(6):1252-7.

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Isolation of a novel tyrosine kinase inhibitor, lavendustin A, from Streptomyces griseolavendus.

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