Inhibition of PDHK isoenzyme assay
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The incorporation of [33P]ATP into the E1 subunit of PDH is measured at 30°C in Mops-K+ buffer in the presence of 100 μM ATP and E2 subunit. Recombinant human proteins are used throughout. Compounds J, K and L are from the same chemical series as AZD7545. IC50 values are means±.E.M. with the number of observations given in parentheses.
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References:
1. Morrell, J. A., Orme, J., Butlin, R. J., Roche, T. E., Mayers, R. M. and Kilgour, E. (2003) AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem Soc Trans. 31, 1168-1170
2. Mayers, R. M., Butlin, R. J., Kilgour, E., Leighton, B., Martin, D., Myatt, J., Orme, J. P. and Holloway, B. R. (2003) AZD7545, a novel inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2), activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats. Biochem Soc Trans. 31, 1165-1167 |