Author

W. J. Zuercher

Listed by name: these papers carry no ORCID for this author, so different people with the same name may be mixed together.

Biology Disciplines

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Pharmacology & Toxicology· 5 Biochemistry· 2 Cancer Biology· 1 Cell Biology· 1 Immunology· 1

Signature Assays, Organisms & Methods

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Approach:experimental assay· 9 Research Focus:drug response / drug discovery· 8 Organism:human· 4 Organism:mouse· 2 Assay:proteomics· 2 Approach:statistical model· 2 Research Focus:benchmarking· 1 Assay:bulk RNA-seq· 1

Frequent Co-Authors

C. I. Wells· 7 shared C. R. M. Asquith· 5 shared J. M. Elkins· 5 shared J. M. Bennett· 4 shared T. M. Willson· 4 shared D. H. Drewry· 3 shared P. H. Godoi· 3 shared T. Laitinen· 3 shared

Activity by Year

2017-2021 · peak 4/yr

Co-Author Collaboration Network

10 top collaborators · 38 mutual co-author links

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7 shared papersPharmacology & Toxicology

C. I. Wells

Mutual co-authors in cluster

Author profile →

10 papers

Recent·Most cited

Temozolomide-induced guanine mutations create exploitable vulnerabilities of guanine-rich DNA and RNA regions in drug resistant gliomas

D. M. Tiek, B. Erdogdu, R. Razaghi, L. Jin, N. Sadowski, C. Alamillo-Ferrer, J. R. Hogg, B. R. Haddad, D. H. Drewry, C. I. Wells, J. E. Pickett, X. Song, A. Goenka, B. Hu, S. L. Goldlust, , R. B. Riggins

This study identifies guanine mutations in TMZ-resistant gliomas that disrupt G4 structures and splice sites, creating vulnerabilities targeted by G4 stabilizers and splicing inhibitors.

bioRxiv · Nov 21, 2021Cancer Biology

Design and analysis of the 4-anilino-quin(az)oline kinase inhibition profiles of GAK/SLK/STK10 using quantitative structure activity relationships

C. R. M. Asquith, T. Laitinen, J. M. Bennett, C. I. Wells, J. M. Elkins, W. J. Zuercher, G. J. Tizzard, A. Poso

The paper designs and synthesizes 4-anilino-quin(az)oline compounds to analyze their kinase inhibition profiles and structure-activity relationships for GAK/SLK/STK10 targets.

bioRxiv · Sep 5, 2019Biochemistry

Inhibition of ErbB kinase signalling promotes resolution of neutrophilic inflammation

L. Prince, S. Renshaw, A. Rahman, K. M. Henry, K. Herman, A. A. R. Thompson, H. Isles, C. Tulotta, D. Sammut, J. Rougeot, N. Khoshaein, A. Reese, K. Higgins, C. Tabor, I. Sabroe, , D. Dockrell

The paper identifies ErbB kinase inhibitors as potential therapies for neutrophilic inflammation by showing they accelerate neutrophil apoptosis in multiple models.

bioRxiv · Aug 19, 2019Immunology

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

C. R. M. Asquith, N. Fleck, C. D. Torrice, D. J. Crona, C. Grundner, W. J. Zuercher

The paper identifies novel anti-tubercular compounds from 4-anilinoquinolines and 4-anilinoquinazolines with high potency and low toxicity.

bioRxiv · Jun 18, 2019Pharmacology & Toxicology

Development of SGC-GAK-1 as an orally active in vivo probe for cyclin G associated kinase through cytochrome P450 inhibition

C. R. M. Asquith, J. M. Bennett, L. Su, T. Latinen, J. M. Elkins, J. E. Pickett, C. I. Wells, Z. Li, T. M. Willson, W. J. Zuercher

The paper develops SGC-GAK-1 as an orally active in vivo probe for GAK by using cytochrome P450 inhibition to improve its metabolic stability and plasma exposure.

bioRxiv · May 7, 2019 · PreprintPharmacology & Toxicology

Design of a GAK/EGFR inhibitor set to interrogate the relationship of EGFR and GAK in chordoma

C. Asquith, K. Naegeli, M. P. East, T. Laitinen, T. M. Havener, C. I. Wells, G. L. Johnson, D. H. Drewry, W. J. Zuercher, D. C. Morris

The paper designs a set of GAK/EGFR inhibitors to study their relationship in chordoma and characterizes their activity in vitro and through target engagement assays.

bioRxiv · Nov 20, 2018Pharmacology & Toxicology

SGC-GAK-1: a chemical probe for cyclin G associated kinase (GAK)

C. R. M. Asquith, B.-T. Berger, J. Wan, J. M. Bennett, M. P. East, J. M. Elkins, O. Fedorov, P. H. Godoi, D. M. Hunter, S. Knapp, S. Mueller, C. I. Wells, H. S. Earp, T. M. Willson, W. J. Zuercher

The paper describes SGC-GAK-1, a selective GAK inhibitor, and identifies a related compound that inhibits RIPK2 without GAK activity, providing tools to study GAK and RIPK2 biology.

bioRxiv · Jul 25, 2018Cell Biology

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

C. R. M. Asquith, T. Laitinen, J. M. Bennett, P. H. Godoi, G. J. Tizzard, J. M. Elkins, T. M. Willson, W. J. Zuercher

The paper identifies 4-anilinoquinolines as potent GAK inhibitors with high selectivity and suggests their potential as tools for studying GAK's role in infectious diseases.

bioRxiv · Apr 11, 2017Pharmacology & Toxicology

Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations

R. M. Counago, C. K. Allerston, P. Savitsky, H. Azevedo, P. H. Godoi, C. I. Wells, A. Mascarello, F. H. de Souza Gama, K. B. Massirer, W. J. Zuercher, C. R. W. Guimaraes, O. Gileadi

The paper identifies BI-D1870 as a starting point for VRK inhibitors and reports co-crystal structures revealing different P-loop conformations in VRK1 and VRK2.

bioRxiv · Mar 2, 2017Biochemistry

Progress Towards a Public Chemogenomic Set for Protein Kinases and a Call for Contributions

D. H. Drewry, C. I. Wells, D. M. Andrews, R. Angell, H. Al-Ali, A. D. Axtman, S. J. Capuzzi, J. M. Elkins, P. Ettmayer, M. Frederiksen, O. Gileadi, N. Gray, A. Hooper, S. Knapp, S. Laufer, , T. M. Willson

The paper shares progress on a kinase chemogenomic set, releases inhibitor profiling data, and calls for community collaboration to complete the set.

bioRxiv · Jan 31, 2017Pharmacology & Toxicology