Literature DB >> 30973735

Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.

Christopher R M Asquith1,2, Kaleb M Naegeli3, Michael P East2, Tuomo Laitinen4, Tammy M Havener3, Carrow I Wells1, Gary L Johnson2, David H Drewry1, William J Zuercher1,5, David C Morris3.   

Abstract

We describe the design of a set of inhibitors to investigate the relationship between cyclin G associated kinase (GAK) and epidermal growth factor receptor (EGFR) in chordoma bone cancers. These compounds were characterized both in vitro and using in cell target engagement assays. The most potent chordoma inhibitors were further characterized in a kinome-wide screen demonstrating narrow spectrum profiles. While we observed a direct correlation between EGFR and antiproliferative effects on chordoma, GAK inhibition appeared to have only a limited effect.

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Year:  2019        PMID： 30973735     DOI： 10.1021/acs.jmedchem.9b00350

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


  10 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 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

3.  Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.

Authors:  Christopher R M Asquith; Neil Fleck; Chad D Torrice; Daniel J Crona; Christoph Grundner; William J Zuercher
Journal:  Bioorg Med Chem Lett       Date:  2019-07-10       Impact factor: 2.823

4.  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

5.  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

6.  Optimization of 4-Anilinoquinolines as Dengue Virus Inhibitors.

Authors:  Pei-Tzu Huang; Sirle Saul; Shirit Einav; Christopher R M Asquith
Journal:  Molecules       Date:  2021-12-03       Impact factor: 4.411

7.  Design, synthesis and biological evaluation of a series of dianilinopyrimidines as EGFR inhibitors.

Authors:  Longjia Yan; Qin Wang; Li Liu; Yi Le
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.051

8.  Numb-associated kinases are required for SARS-CoV-2 infection and are cellular targets for antiviral strategies.

Authors:  Marwah Karim; Sirle Saul; Luca Ghita; Malaya Kumar Sahoo; Chengjin Ye; Nishank Bhalla; Chieh-Wen Lo; Jing Jin; Jun-Gyu Park; Belén Martinez-Gualda; Michael Patrick East; Gary L Johnson; Benjamin A Pinsky; Luis Martinez-Sobrido; Christopher R M Asquith; Aarthi Narayanan; Steven De Jonghe; Shirit Einav
Journal:  Antiviral Res       Date:  2022-06-20       Impact factor: 10.103

9.  The cyclin G-associated kinase (GAK) inhibitor SGC-GAK-1 inhibits neurite outgrowth and synapse formation.

Authors:  Jun Egawa; Reza K Arta; Vance P Lemmon; Melissa Muños-Barrero; Yan Shi; Michihiro Igarashi; Toshiyuki Someya
Journal:  Mol Brain       Date:  2022-07-26       Impact factor: 4.399

10.  Optimization of the 4-anilinoquin(az)oline scaffold as epidermal growth factor receptor (EGFR) inhibitors for chordoma utilizing a toxicology profiling assay platform.

Authors:  Andrew A Bieberich; Tuomo Laitinen; Kaitlyn Maffuid; Raymond O Fatig; Chad D Torrice; David C Morris; Daniel J Crona; Christopher R M Asquith
Journal:  Sci Rep       Date:  2022-07-27       Impact factor: 4.996
  10 in total

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