Literature DB >> 31129055

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

Christopher R M Asquith1, Daniel K Treiber2, William J Zuercher3.   

Abstract

We demonstrate an innovative approach for optimization of kinase inhibitor potency and selectivity utilising kinase mini-panels and kinome-wide panels. We present a focused case study on development of a selective inhibitor of cyclin G associated kinase (GAK) using the quin(az)oline inhibitor chemotype. These results exemplify a versatile, efficient approach to drive kinome selectivity during inhibitor development programs.
Copyright © 2019 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  4-Anilinoquinazoline; 4-anilinoquinoline; Cyclin G associated kinase (GAK); Kinome selectivity; Mini-kinome panel

Year:  2019        PMID： 31129055     DOI： 10.1016/j.bmcl.2019.05.025

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 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.  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

8.  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

9.  Hit Identification of a Novel Quinazoline Sulfonamide as a Promising EphB3 Inhibitor: Design, Virtual Combinatorial Library, Synthesis, Biological Evaluation, and Docking Simulation Studies.

Authors:  Kyeong Lee; Hossam Nada; Hyun Jung Byun; Chang Hoon Lee; Ahmed Elkamhawy
Journal:  Pharmaceuticals (Basel)       Date:  2021-11-30
  9 in total

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