International Journal of Molecular Sciences (Jan 2021)
The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification
- Carrow I. Wells,
- Hassan Al-Ali,
- David M. Andrews,
- Christopher R. M. Asquith,
- Alison D. Axtman,
- Ivan Dikic,
- Daniel Ebner,
- Peter Ettmayer,
- Christian Fischer,
- Mathias Frederiksen,
- Robert E. Futrell,
- Nathanael S. Gray,
- Stephanie B. Hatch,
- Stefan Knapp,
- Ulrich Lücking,
- Michael Michaelides,
- Caitlin E. Mills,
- Susanne Müller,
- Dafydd Owen,
- Alfredo Picado,
- Kumar S. Saikatendu,
- Martin Schröder,
- Alexandra Stolz,
- Mariana Tellechea,
- Brandon J. Turunen,
- Santiago Vilar,
- Jinhua Wang,
- William J. Zuercher,
- Timothy M. Willson,
- David H. Drewry
Affiliations
- Carrow I. Wells
- Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
- Hassan Al-Ali
- The Miami Project to Cure Paralysis, Peggy and Harold Katz Family Drug Discovery Center, Sylvester Comprehensive Cancer Center, Departments of Neurological Surgery and Medicine, University of Miami Miller School of Medicine, Miami, FL 33136, USA
- David M. Andrews
- AstraZeneca, Darwin Building, Cambridge Science Park, Cambridge CB4 0WG, UK
- Christopher R. M. Asquith
- Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
- Alison D. Axtman
- Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
- Ivan Dikic
- Institute of Biochemistry 2, Faculty of Medicine, Goethe University Frankfurt, Theodor-Stern-Kai 7, 60438 Frankfurt am Main, Germany
- Daniel Ebner
- Nuffield Department of Medicine, Target Discovery Institute, University of Oxford, Oxford OX3 7FZ, UK
- Peter Ettmayer
- Boehringer Ingelheim RCV GmbH & Co KG, 1121 Vienna, Austria
- Christian Fischer
- MSD, 33 Avenue Louis Pasteur, Boston, MA 02115, USA
- Mathias Frederiksen
- Novartis Institutes for BioMedical Research, Novartis Campus, 4056 Basel, Switzerland
- Robert E. Futrell
- Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
- Nathanael S. Gray
- Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA
- Stephanie B. Hatch
- MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford OX3 7XB, UK
- Stefan Knapp
- Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany
- Ulrich Lücking
- Bayer Pharma AG, Drug Discovery, Müllerstrasse 178, 13353 Berlin, Germany
- Michael Michaelides
- Oncology Discovery, AbbVie, 1 North Waukegan Road, North Chicago, IL 60064, USA
- Caitlin E. Mills
- Laboratory of Systems Pharmacology, Department of Systems Biology, Harvard Medical School, Boston, MA 02115, USA
- Susanne Müller
- Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany
- Dafydd Owen
- Discovery Network Group, Pfizer Medicine Design, Cambridge, MA 02139, USA
- Alfredo Picado
- Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
- Kumar S. Saikatendu
- Global Research Externalization, Takeda California, Inc., 9625 Towne Center Drive, San Diego, CA 92121, USA
- Martin Schröder
- Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Str. 15, 60438 Frankfurt am Main, Germany
- Alexandra Stolz
- Institute of Biochemistry 2, Faculty of Medicine, Goethe University Frankfurt, Theodor-Stern-Kai 7, 60438 Frankfurt am Main, Germany
- Mariana Tellechea
- Institute of Biochemistry 2, Faculty of Medicine, Goethe University Frankfurt, Theodor-Stern-Kai 7, 60438 Frankfurt am Main, Germany
- Brandon J. Turunen
- GlaxoSmithKline, Chemical Biology, 1250 S Collegeville Rd, Collegeville, PA 19426, USA
- Santiago Vilar
- Truvitech LLC, Miami, FL 33136, USA
- Jinhua Wang
- Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115, USA
- William J. Zuercher
- Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
- Timothy M. Willson
- Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
- David H. Drewry
- Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
- DOI
- https://doi.org/10.3390/ijms22020566
- Journal volume & issue
-
Vol. 22,
no. 2
p. 566
Abstract
We describe the assembly and annotation of a chemogenomic set of protein kinase inhibitors as an open science resource for studying kinase biology. The set only includes inhibitors that show potent kinase inhibition and a narrow spectrum of activity when screened across a large panel of kinase biochemical assays. Currently, the set contains 187 inhibitors that cover 215 human kinases. The kinase chemogenomic set (KCGS), current Version 1.0, is the most highly annotated set of selective kinase inhibitors available to researchers for use in cell-based screens.
Keywords
