Literature DB >> 30768268

SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK).

Christopher R M Asquith, Benedict-Tilman Berger1,2, Jing Wan, James M Bennett3, Stephen J Capuzzi, Daniel J Crona, David H Drewry, Michael P East, Jonathan M Elkins3,4, Oleg Fedorov3, Paulo H Godoi4, Debra M Hunter, Stefan Knapp1,2, Susanne Müller1, Chad D Torrice, Carrow I Wells, H Shelton Earp, Timothy M Willson, William J Zuercher.   

Abstract

We describe SGC-GAK-1 (11), a potent, selective, and cell-active inhibitor of cyclin G-associated kinase (GAK), together with a structurally related negative control SGC-GAK-1N (14). 11 was highly selective in an in vitro kinome-wide screen, but cellular engagement assays defined RIPK2 as a collateral target. We identified 18 as a potent RIPK2 inhibitor lacking GAK activity. Together, this chemical probe set can be used to interrogate GAK cellular biology.

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Year:  2019        PMID： 30768268      PMCID： PMC6567991          DOI： 10.1021/acs.jmedchem.8b01213

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  26 in total

1.  Structure, expression, and chromosomal localization of human GAK.

Authors:  S H Kimura; H Tsuruga; N Yabuta; Y Endo; H Nojima
Journal:  Genomics       Date:  1997-09-01       Impact factor: 5.736

2.  Cyclin G-associated kinase: a novel androgen receptor-interacting transcriptional coactivator that is overexpressed in hormone refractory prostate cancer.

Authors:  Mira R Ray; Latif A Wafa; Helen Cheng; Robert Snoek; Ladan Fazli; Martin Gleave; Paul S Rennie
Journal:  Int J Cancer       Date:  2006-03-01       Impact factor: 7.396

Review 3.  Multiple roles of auxilin and hsc70 in clathrin-mediated endocytosis.

Authors:  Evan Eisenberg; Lois E Greene
Journal:  Traffic       Date:  2007-05-04       Impact factor: 6.215

4.  GAK, a regulator of clathrin-mediated membrane traffic, also controls centrosome integrity and chromosome congression.

Authors:  Hiroyuki Shimizu; Ippei Nagamori; Norikazu Yabuta; Hiroshi Nojima
Journal:  J Cell Sci       Date:  2009-08-04       Impact factor: 5.285

5.  Identification and Optimization of 4-Anilinoquinolines as Inhibitors of Cyclin G Associated Kinase.

Authors:  Christopher R M Asquith; Tuomo Laitinen; James M Bennett; Paulo H Godoi; Michael P East; Graham J Tizzard; Lee M Graves; Gary L Johnson; Ronna E Dornsife; Carrow I Wells; Jonathan M Elkins; Timothy M Willson; William J Zuercher
Journal:  ChemMedChem       Date:  2017-11-27       Impact factor: 3.466

6.  The promise and peril of chemical probes.

Authors:  Cheryl H Arrowsmith; James E Audia; Christopher Austin; Jonathan Baell; Jonathan Bennett; Julian Blagg; Chas Bountra; Paul E Brennan; Peter J Brown; Mark E Bunnage; Carolyn Buser-Doepner; Robert M Campbell; Adrian J Carter; Philip Cohen; Robert A Copeland; Ben Cravatt; Jayme L Dahlin; Dashyant Dhanak; Aled M Edwards; Mathias Frederiksen; Stephen V Frye; Nathanael Gray; Charles E Grimshaw; David Hepworth; Trevor Howe; Kilian V M Huber; Jian Jin; Stefan Knapp; Joanne D Kotz; Ryan G Kruger; Derek Lowe; Mary M Mader; Brian Marsden; Anke Mueller-Fahrnow; Susanne Müller; Ronan C O'Hagan; John P Overington; Dafydd R Owen; Saul H Rosenberg; Bryan Roth; Brian Roth; Ruth Ross; Matthieu Schapira; Stuart L Schreiber; Brian Shoichet; Michael Sundström; Giulio Superti-Furga; Jack Taunton; Leticia Toledo-Sherman; Chris Walpole; Michael A Walters; Timothy M Willson; Paul Workman; Robert N Young; William J Zuercher
Journal:  Nat Chem Biol       Date:  2015-08       Impact factor: 15.040

7.  Neonatal lethality in knockout mice expressing the kinase-dead form of the gefitinib target GAK is caused by pulmonary dysfunction.

Authors:  Hiroe Tabara; Yoko Naito; Akihiko Ito; Asako Katsuma; Minami A Sakurai; Shouichi Ohno; Hiroyuki Shimizu; Norikazu Yabuta; Hiroshi Nojima
Journal:  PLoS One       Date:  2011-10-12       Impact factor: 3.240

8.  Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement.

Authors:  James D Vasta; Cesear R Corona; Jennifer Wilkinson; Chad A Zimprich; James R Hartnett; Morgan R Ingold; Kristopher Zimmerman; Thomas Machleidt; Thomas A Kirkland; Kristin G Huwiler; Rachel Friedman Ohana; Michael Slater; Paul Otto; Mei Cong; Carrow I Wells; Benedict-Tilman Berger; Thomas Hanke; Carina Glas; Ke Ding; David H Drewry; Kilian V M Huber; Timothy M Willson; Stefan Knapp; Susanne Müller; Poncho L Meisenheimer; Frank Fan; Keith V Wood; Matthew B Robers
Journal:  Cell Chem Biol       Date:  2017-11-22       Impact factor: 8.116

9.  Structure of cyclin G-associated kinase (GAK) trapped in different conformations using nanobodies.

Authors:  Apirat Chaikuad; Tracy Keates; Cécile Vincke; Melanie Kaufholz; Michael Zenn; Bastian Zimmermann; Carlos Gutiérrez; Rong-Guang Zhang; Catherine Hatzos-Skintges; Andrzej Joachimiak; Serge Muyldermans; Friedrich W Herberg; Stefan Knapp; Susanne Müller
Journal:  Biochem J       Date:  2014-04-01       Impact factor: 3.857

Review 10.  Parkinson's disease-implicated kinases in the brain; insights into disease pathogenesis.

Authors:  Nicolas Dzamko; Jinxia Zhou; Yue Huang; Glenda M Halliday
Journal:  Front Mol Neurosci       Date:  2014-06-24       Impact factor: 5.639
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  20 in total

1.  Quinazoline-Based Antivirulence Compounds Selectively Target Salmonella PhoP/PhoQ Signal Transduction System.

Authors:  María Ayelén Carabajal; Christopher R M Asquith; Tuomo Laitinen; Graham J Tizzard; Lucía Yim; Analía Rial; José A Chabalgoity; William J Zuercher; Eleonora García Véscovi
Journal:  Antimicrob Agents Chemother       Date:  2019-12-20       Impact factor: 5.191

2.  Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses.

Authors:  David H Drewry; Frances M Potjewyd; Armin Bayati; Jeffery L Smith; Rebekah J Dickmander; Stefanie Howell; Sharon Taft-Benz; Sophia M Min; Mohammad Anwar Hossain; Mark Heise; Peter S McPherson; Nathaniel J Moorman; Alison D Axtman
Journal:  J Med Chem       Date:  2022-09-16       Impact factor: 8.039

3.  CDK11 regulates pre-mRNA splicing by phosphorylation of SF3B1.

Authors:  Milan Hluchý; Pavla Gajdušková; Igor Ruiz de Los Mozos; Michal Rájecký; Michael Kluge; Benedict-Tilman Berger; Zuzana Slabá; David Potěšil; Elena Weiß; Jernej Ule; Zbyněk Zdráhal; Stefan Knapp; Kamil Paruch; Caroline C Friedel; Dalibor Blazek
Journal:  Nature       Date:  2022-09-14       Impact factor: 69.504

4.  Identification of 4-Anilinoquin(az)oline as a Cell-Active Protein Kinase Novel 3 (PKN3) Inhibitor Chemotype.

Authors:  Christopher R M Asquith; Louisa Temme; Michael P East; Tuomo Laitinen; Julie Pickett; Frank E Kwarcinski; Parvathi Sinha; Carrow I Wells; Gary L Johnson; Reena Zutshi; David H Drewry
Journal:  ChemMedChem       Date:  2022-05-09       Impact factor: 3.540

5.  Development of a potent and selective chemical probe for the pleiotropic kinase CK2.

Authors:  Carrow I Wells; David H Drewry; Julie E Pickett; Amelie Tjaden; Andreas Krämer; Susanne Müller; Laszlo Gyenis; Daniel Menyhart; David W Litchfield; Stefan Knapp; Alison D Axtman
Journal:  Cell Chem Biol       Date:  2021-01-22       Impact factor: 8.116

6.  SGC-AAK1-1: A Chemical Probe Targeting AAK1 and BMP2K.

Authors:  Carrow Wells; Rafael M Couñago; Juanita C Limas; Tuanny L Almeida; Jeanette Gowen Cook; David H Drewry; Jonathan M Elkins; Opher Gileadi; Nirav R Kapadia; Alvaro Lorente-Macias; Julie E Pickett; Alexander Riemen; Roberta R Ruela-de-Sousa; Timothy M Willson; Cunyu Zhang; William J Zuercher; Reena Zutshi; Alison D Axtman
Journal:  ACS Med Chem Lett       Date:  2019-10-23       Impact factor: 4.632

7.  New Insights into 4-Anilinoquinazolines as Inhibitors of Cardiac Troponin I-Interacting Kinase (TNNi3K).

Authors:  Christopher R M Asquith; Tuomo Laitinen; Carrow I Wells; Graham J Tizzard; William J Zuercher
Journal:  Molecules       Date:  2020-04-07       Impact factor: 4.411

8.  Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK).

Authors:  Christopher R M Asquith; James M Bennett; Lianyong Su; Tuomo Laitinen; Jonathan M Elkins; Julie E Pickett; Carrow I Wells; Zengbiao Li; Timothy M Willson; William J Zuercher
Journal:  Molecules       Date:  2019-11-06       Impact factor: 4.411

9.  Host kinase CSNK2 is a target for inhibition of pathogenic β-coronaviruses including SARS-CoV-2.

Authors:  Xuan Yang; Rebekah J Dickmander; Armin Bayati; Sharon A Taft-Benz; Jeffery L Smith; Carrow I Wells; Emily A Madden; Jason W Brown; Erik M Lenarcic; Boyd L Yount; Edcon Chang; Alison D Axtman; Ralph S Baric; Mark T Heise; Peter S McPherson; Nathaniel J Moorman; Timothy M Willson
Journal:  bioRxiv       Date:  2022-01-26

Review 10.  Medicinal chemistry strategies toward host targeting antiviral agents.

Authors:  Xingyue Ji; Zhuorong Li
Journal:  Med Res Rev       Date:  2020-02-14       Impact factor: 12.944
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