Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase
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Asquith, Christopher R. M.; Laitinen, Tuomo; Bennett, James M.; Godoi, Paulo H.; Tizzard, Graham J.; Elkins, Jonathan M.; Willson, Timothy M.; +1 Authors
Asquith, Christopher R. M.; Laitinen, Tuomo; Bennett, James M.; Godoi, Paulo H.; Tizzard, Graham J.; Elkins, Jonathan M.; Willson, Timothy M.; Zuercher, William J.;
Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase
ABSTRACT 4-Anilinoquinolines were identified as potent and narrow spectrum inhibitors of the cyclin G associated kinase (GAK), an important regulator of viral and bacterial entry into host cells. Optimization of the 4-anilino group and the 6,7-quinoline substituents produced GAK inhibitors with nanomolar activity and over 50,000-fold selectivity relative to other members of the numb-associated kinase (NAK) sub-family. These compounds may be useful tools to explore the therapeutic potential of GAK in prevention of a broad range of infectious diseases.
- University of North Carolina at Chapel Hill United States
- State University of Campinas Brazil
- University of Eastern Finland Finland
- University of Oxford United Kingdom
- University of Southampton United Kingdom
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These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
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