PT  - JOURNAL ARTICLE
AU  - Christopher R. M. Asquith
AU  - Tuomo Laitinen
AU  - James M. Bennett
AU  - Paulo H. Godoi
AU  - Graham J. Tizzard
AU  - Jonathan M. Elkins
AU  - Timothy M. Willson
AU  - William J. Zuercher
TI  - Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase
AID  - 10.1101/117630
DP  - 2017 Jan 01
TA  - bioRxiv
PG  - 117630
4099  - http://biorxiv.org/content/early/2017/04/11/117630.short
4100  - http://biorxiv.org/content/early/2017/04/11/117630.full
AB  - 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.