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2011
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Discovery of a potent and highly selective PDK1 inhibitor via fragment-based drug discovery.
Discovery of a potent and highly selective PDK1 inhibitor via fragment-based drug discovery.
Erlanson, D.A., Arndt, J.W., Cancilla, M.T., Cao, K., Elling, R.A., English, N., Friedman, J., Hansen, S.K., Hession, C., Joseph, I., Kumaravel, G., Lee, W.C., Lind, K.E., McDowell, R.S., Miatkowski, K., Nguyen, C., Nguyen, T.B., Park, S., Pathan, N., Penny, D.M., Romanowski, M.J., Scott, D., Silvian, L., Simmons, R.L., Tangonan, B.T., Yang, W., Sun, L.
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Journal
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Bioorg Med Chem Lett.
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Species
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Analytes Measured
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Akt
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Matrix Tested
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PC-3 cell lysates
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Abstract
We report the use of a fragment-based lead discovery method, Tethering with extenders, to discover a pyridinone fragment that binds in an adaptive site of the protein PDK1. With subsequent medicinal chemistry, this led to the discovery of a potent and highly selective inhibitor of PDK1, which binds in the 'DFG-out' conformation.
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