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- W4312019027 endingPage "139" @default.
- W4312019027 startingPage "122" @default.
- W4312019027 abstract "Now entering its fourth decade, research on the biological function, small molecule inhibition, and disease relevance of the three known isoforms of protein kinase D, PKD1, PKD2, and PKD3, has entered a mature development stage. This mini-perspective focuses on the medicinal chemistry that provided a structurally diverse set of mainly active site inhibitors, which, for a brief time period, moved through preclinical development stages but have yet to be tested in clinical trials. In particular, between 2006 and 2012, a rapid expansion of synthetic efforts led to several moderately to highly PKD-selective chemotypes but did not yet achieve PKD subtype selectivity or resolve general toxicity and pharmacokinetic challenges. In addition to cancer, other unresolved medical needs in cardiovascular, inflammatory, and metabolic diseases would, however, benefit from a renewed focus on potent and selective PKD modulators." @default.
- W4312019027 created "2023-01-03" @default.
- W4312019027 creator A5009584633 @default.
- W4312019027 creator A5018024103 @default.
- W4312019027 date "2022-12-20" @default.
- W4312019027 modified "2023-10-03" @default.
- W4312019027 title "Small Molecule Inhibitors of Protein Kinase D: Early Development, Current Approaches, and Future Directions" @default.
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- W4312019027 doi "https://doi.org/10.1021/acs.jmedchem.2c01599" @default.
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- W4312019027 hasPublicationYear "2022" @default.
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