Novel protein kinase D inhibitors cause potent arrest in prostate cancer cell growth and motility |
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| Authors: | Courtney R LaValle Karla Bravo-Altamirano Karthik V Giridhar Jun Chen Elizabeth Sharlow John S Lazo Peter Wipf Q Jane Wang |
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| Institution: | (1) Department of Pharmacology and Chemical Biology, University of Pittsburgh, 15261 Pittsburgh, Pennsylvania, USA;(2) University of Pittsburgh Drug Discovery Institute, University of Pittsburgh, 15261 Pittsburgh, Pennsylvania, USA;(3) Department of Chemistry, University of Pittsburgh, 15261 Pittsburgh, Pennsylvania, USA |
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| Abstract: | Background Protein kinase D (PKD) has been implicated in a wide range of cellular processes and pathological conditions including cancer.
However, targeting PKD therapeutically and dissecting PKD-mediated cellular responses remains difficult due to lack of a potent
and selective inhibitor. Previously, we identified a novel pan-PKD inhibitor, CID755673, with potency in the upper nanomolar
range and high selectivity for PKD. In an effort to further enhance its selectivity and potency for potential in vivo application, small molecule analogs of CID755673 were generated by modifying both the core structure and side-chains. |
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