scholarly journals Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase

ChemMedChem ◽  
2017 ◽  
Vol 13 (1) ◽  
pp. 48-66 ◽  
Author(s):  
Christopher R. M. Asquith ◽  
Tuomo Laitinen ◽  
James M. Bennett ◽  
Paulo H. Godoi ◽  
Michael P. East ◽  
...  
Keyword(s):  
Cyclin G

scholarly journals More about Cyclin G from flies

Cell Cycle ◽  
2011 ◽  
Vol 10 (8) ◽  
pp. 1187-1187
Author(s):  
Jacques Montagne
Keyword(s):  
Cyclin G

scholarly journals Isothiazolo[4,3-b]pyridines as inhibitors of cyclin G associated kinase: synthesis, structure–activity relationship studies and antiviral activity

MedChemComm ◽  
2015 ◽  
Vol 6 (9) ◽  
pp. 1666-1672 ◽  
Author(s):  
Jiahong Li ◽  
Sona Kovackova ◽  
Szuyuan Pu ◽  
Jef Rozenski ◽  
Steven De Jonghe ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
Cyclin G

Starting from a known isothiazolo[4,3-b]pyridine scaffold, different series of novel, potent GAK ligands were synthesized.

Cyclin G-Associated Kinase

2008 ◽  
pp. 795-798
Author(s):  
Mira R. Ray ◽  
Paul S. Rennie
Keyword(s):  
Cyclin G

scholarly journals Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK)

2019 ◽  
Vol 29 (14) ◽  
pp. 1727-1731 ◽  
Author(s):  
Christopher R.M. Asquith ◽  
Daniel K. Treiber ◽  
William J. Zuercher
Keyword(s):  
Cyclin G

Multiple Roles for Cyclin G-Associated Kinase in Clathrin-Mediated Sorting Events

Traffic ◽  
2005 ◽  
Vol 6 (12) ◽  
pp. 1103-1113 ◽  
Author(s):  
Claire X. Zhang ◽  
Åsa E. Y. Engqvist-Goldstein ◽  
Sebastien Carreno ◽  
David J. Owen ◽  
Elizabeth Smythe ◽  
...  
Keyword(s):  
Multiple Roles ◽  
Cyclin G

scholarly journals Cyclin G Functions as a Positive Regulator of Growth and Metabolism in Drosophila

PLoS Genetics ◽  
2015 ◽  
Vol 11 (8) ◽  
pp. e1005440 ◽  
Author(s):  
Patrick Fischer ◽  
Martina K. La Rosa ◽  
Adriana Schulz ◽  
Anette Preiss ◽  
Anja C. Nagel
Keyword(s):  
Positive Regulator ◽  
Cyclin G

scholarly journals Essential Role of Cyclin-G–associated Kinase (Auxilin-2) in Developing and Mature Mice

2008 ◽  
Vol 19 (7) ◽  
pp. 2766-2776 ◽  
Author(s):  
Dong-won Lee ◽  
Xiaohong Zhao ◽  
Yang-In Yim ◽  
Evan Eisenberg ◽  
Lois E. Greene
Keyword(s):  
Essential Gene ◽  
Inducible Promoter ◽  
Cre Recombinase ◽  
Conditional Knockout ◽  
Mouse Embryonic Fibroblasts ◽  
Coated Pits ◽  
Embryonic Fibroblasts ◽  
Adult Mice ◽  
Cyclin G

Hsc70 with its cochaperone, either auxilin or GAK, not only uncoats clathrin-coated vesicles but also acts as a chaperone during clathrin-mediated endocytosis. However, because synaptojanin is also involved in uncoating, it is not clear whether GAK is an essential gene. To answer this question, GAK conditional knockout mice were generated and then mated to mice expressing Cre recombinase under the control of the nestin, albumin, or keratin-14 promoters, all of which turn on during embryonic development. Deletion of GAK from brain, liver, or skin dramatically altered the histology of these tissues, causing the mice to die shortly after birth. Furthermore, by expressing a tamoxifen-inducible promoter to express Cre recombinase we showed that deletion of GAK caused lethality in adult mice. Mouse embryonic fibroblasts in which the GAK was disrupted showed a lack of clathrin-coated pits and a complete block in clathrin-mediated endocytosis. We conclude that GAK deletion blocks development and causes lethality in adult animals by disrupting clathrin-mediated endocytosis.

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