The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification

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 bioch...

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Published inInternational journal of molecular sciences Vol. 22; no. 2; p. 566
Main Authors Wells, Carrow I, Al-Ali, Hassan, Andrews, David M, Asquith, Christopher R M, Axtman, Alison D, Dikic, Ivan, Ebner, Daniel, Ettmayer, Peter, Fischer, Christian, Frederiksen, Mathias, Futrell, Robert E, Gray, Nathanael S, Hatch, Stephanie B, Knapp, Stefan, Lücking, Ulrich, Michaelides, Michael, Mills, Caitlin E, Müller, Susanne, Owen, Dafydd, Picado, Alfredo, Saikatendu, Kumar S, Schröder, Martin, Stolz, Alexandra, Tellechea, Mariana, Turunen, Brandon J, Vilar, Santiago, Wang, Jinhua, Zuercher, William J, Willson, Timothy M, Drewry, David H
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 08.01.2021
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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.
AbstractList 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.
Author Al-Ali, Hassan
Gray, Nathanael S
Tellechea, Mariana
Fischer, Christian
Müller, Susanne
Axtman, Alison D
Owen, Dafydd
Mills, Caitlin E
Vilar, Santiago
Saikatendu, Kumar S
Futrell, Robert E
Knapp, Stefan
Frederiksen, Mathias
Lücking, Ulrich
Ettmayer, Peter
Schröder, Martin
Wang, Jinhua
Drewry, David H
Ebner, Daniel
Wells, Carrow I
Stolz, Alexandra
Picado, Alfredo
Asquith, Christopher R M
Andrews, David M
Michaelides, Michael
Willson, Timothy M
Dikic, Ivan
Zuercher, William J
Turunen, Brandon J
Hatch, Stephanie B
AuthorAffiliation 3 Truvitech LLC, Miami, FL 33136, USA; santiago@truvitech.com
16 Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany
9 Boehringer Ingelheim RCV GmbH & Co KG, 1121 Vienna, Austria; peter.ettmayer@boehringer-ingelheim.com
14 MRC Oxford Institute for Radiation Oncology, Department of Oncology, University of Oxford, Roosevelt Drive, Oxford OX3 7XB, UK; stephanie.hatch@ndm.ox.ac.uk
17 Bayer Pharma AG, Drug Discovery, Müllerstrasse 178, 13353 Berlin, Germany; ulrich.luecking@forxtherapeutics.com
22 GlaxoSmithKline, Chemical Biology, 1250 S Collegeville Rd, Collegeville, PA 19426, USA; brandon.j.turunen@gsk.com
15 Structural Genomics Consortium, Buchmann Institute for Molecular Life Sciences, Goethe University Frankfurt, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany
2 The Miami Project to Cure Paralysis, Peggy and Harold Katz Family Drug Discovery Center, Sylvester Comprehensive Cancer Center, Departments of Neur
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BackLink https://www.ncbi.nlm.nih.gov/pubmed/33429995$$D View this record in MEDLINE/PubMed
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2021 by the authors. 2021
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Issue 2
Keywords druggable genome
kinase inhibitor
chemogenomic set
drug discovery
KCGS
phenotypic screening
understudied kinase
protein kinase
small molecules
Language English
License https://creativecommons.org/licenses/by/4.0
Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
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SubjectTerms Annotations
Binding sites
Biology
chemogenomic set
Drug Discovery
Experiments
Humans
Initiatives
KCGS
kinase inhibitor
Kinases
Medical research
Pharmaceutical industry
phenotypic screening
protein kinase
Protein kinase inhibitors
Protein Kinase Inhibitors - chemistry
Protein Kinase Inhibitors - therapeutic use
Protein Serine-Threonine Kinases - antagonists & inhibitors
Protein Serine-Threonine Kinases - chemistry
Small Molecule Libraries - chemistry
Small Molecule Libraries - therapeutic use
small molecules
Structure-Activity Relationship
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Title The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification
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https://search.proquest.com/docview/2477260845
https://pubmed.ncbi.nlm.nih.gov/PMC7826789
https://doaj.org/article/98332da56c7a48cebc35217b75e5dc25
Volume 22
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