Genistein protein kinases

Genistein, a specific inhibitor of tyrosine-specific protein kinases. JBiol Chem. 262 5592-5. 

GAO Y H and YAMAGUCHI M (2000) Suppressive effect of genistein on rat bone osteoclasts Involvement of protein kinase inhibition and protein tyrosine phosphatase activation. Int J Mol Med 5, 261-7. 

The mechanism of action proposed is based on a direct binding to the channel and the following partial block of the ATP-binding pocket of CFTR (French et al., 1997), a mechanism similar to that used by genistein to inhibit the activity of other ATP-utilizing enzymes such as protein kinases and topoisomerase II (Polkowski and Mazurek, 2000 and refs therein). The selection of flavonoid compounds or the development of synthetic drugs reasonably selective for CFTR activation might be an area for future clinical trials. 

Protein Kinase Inhibitors Pseudosubstrate-based peptide inhibitors, 201, 287 utilization of the inhibitor protein of adenosine cyclic monophosphate-dependent protein kinase, and peptides derived from it, as tools to study adenosine cyclic monophosphate-mediated cellular processes, 201, 304 use of sphingosine as inhibitor of protein kinase C, 201, 316 properties and use of H-series compounds as protein kinase inhibitors, 201, 328 use and specificity of staurosporine, UCN-01, and calphostin C as protein kinase inhibitors, 201, 340 inhibition of protein-tyrosine kinases by tyrphostins, 201, 347 use and specificity of genistein as inhibitor of protein-tyrosine kinases, 201, 362 use and selectivity of herbimycin a as inhibitor of protein-tyrosine kinases,... 

Akiyama, T., Ishida, J., Nakagawa, S., Ogawara, H., Watanabe, S., Itoh, N., Shibuya, M., and Eukami, Y., Genistein, a specific inhibitor of tyrosine-specific protein kinases, J. Biol. Chem., 262, 5592, 1987. 

Akiyama T, Ishida J, Nakagawa S et al. Genistein, a specific inhibitor of t5Tosine-specific protein kinases. J. Biol Chem. 262, 5592-5595, 1987. 

Naturally occurring flavonoids, such as quercetin and genistein, inhibit tyrosine kinase activity by competing with ATP (Akiyama et al., 1987), and have been shown to inhibit cAMP-dependent protein kinase, PKC, and other ATP-requiring enzymes (Gazit et al.,... 

Daidzein and genistein have been most intensively investigated because of their high levels of occurrence in soybean, a widely used animal feedstuff and a component of traditional Asian diets consumed daily in high quantities by Japanese [10] and Chinese populations [8, 11]. The consumption of products derived from soy has, therefore, been considered as the major dietary factor contributing to the lower rates of hormone-dependent diseases, including breast, prostate, and colon cancers and coronary heart disease, in many Asian countries [12-14]. Almost 10 years after Akiyama et al. [15] first identified genistein as a tyrosine protein kinase inhibitor [15], it was entered into clinical chemoprevention trials in 1996 [16, 17], followed by formal human trials as a treatment for acute lymphoblastic leukemia and breast cancer [18-20]. 

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