Lee R H, Slate D L, Moretti R, Alvi K A, Crews P
Institute of Cancer and Developmental Biology, Syntex Research, Palo Alto, CA 94304.
Biochem Biophys Res Commun. 1992 Apr 30;184(2):765-72. doi: 10.1016/0006-291x(92)90656-6.
The marine polyketide natural product, halenaquinone, was shown to be an irreversible inhibitor of pp60v-src, the oncogenic protein tyrosine kinase encoded by the Rous sarcoma virus. This compound had an IC50 of approximately 1.5 microM against pp60v-src and also inhibited the ligand-stimulated kinase activity of the human epidermal growth factor receptor with an IC50 of approximately 19 microM. Halenaquinone blocked the proliferation of a number of cultured cell lines, including several transformed by oncogenic protein tyrosine kinases. Halenaquinol, xestoquinone, halenaquinol sulfate, and several simple synthetic quinone analogs were also shown to inhibit pp60v-src.
