573675-27-1Relevant articles and documents
Selective inhibitors of cyclin G associated kinase (GAK) as anti-hepatitis C agents
Kovackova, Sona,Chang, Lei,Bekerman, Elena,Neveu, Gregory,Barouch-Bentov, Rina,Chaikuad, Apirat,Heroven, Christina,?ála, Michal,De Jonghe, Steven,Knapp, Stefan,Einav, Shirit,Herdewijn, Piet
, p. 3393 - 3410 (2015)
Cyclin G associated kinase (GAK) emerged as a promising drug target for the treatment of viral infections. However, no potent and selective GAK inhibitors have been reported in the literature to date. This paper describes the discovery of isothiazolo[5,4-
A Scaffold-Hopping Strategy toward the Identification of Inhibitors of Cyclin G Associated Kinase
Wouters, Randy,Tian, Junjun,Herdewijn, Piet,De Jonghe, Steven
, p. 237 - 254 (2019/01/08)
We recently reported the discovery of isothiazolo[4,3-b]pyridine-based inhibitors of cyclin G associated kinase (GAK) displaying low nanomolar binding affinity for GAK and demonstrating broad-spectrum antiviral activity. To come up with novel core structures that act as GAK inhibitors, a scaffold-hopping approach was applied starting from two different isothiazolo[4,3-b]pyridines. In total, 13 novel 5,6- and 6,6-fused bicyclic heteroaromatic scaffolds were synthesized. Four of them displayed GAK affinity with Kd values in the low micromolar range that can serve as chemical starting points for the discovery of GAK inhibitors based on a different scaffold.
GAK MODULATORS AS ANTIVIRALS
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Page/Page column 31; 32, (2016/02/18)
The present invention relates to the use of a class of novel isothiazolo[4,3-b]pyridine derivatives as well as to pharmaceutical compositions comprising one or more of said isothiazolo[4,3- b]pyridine derivatives and one or more pharmaceutically acceptable excipients as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as viral diseases.