David H. Drewry, Carrow I. Wells, David M. Andrews, Richard Angell, Hassan Al-Ali, Alison D. Axtman, Stephen J. Capuzz, Jonathan M. Elkins, Peter Ettmayer, Mathias Frederiksen, Opher Gileadi, Nathanael S. Gray, Alice Hooper, Stefan Knapp, Stefan Laufer, Ulrich Lücking, Michael Michaelides, Susanne Müller, Eugene Muratov, R. Aldrin Denny, Kumar S. Saikatendu, Daniel K. Treiber, William J. Zuercher, Timothy M. Willson
- Protein kinases are highly tractable targets for drug discovery. However, the biological function and therapeutic potential of the majority of the 500+ human protein kinases remains unknown. We have developed physical and virtual collections of small molecule inhibitors, which we call chemogenomic sets, that are designed to inhibit the catalytic function of almost half the human protein kinases. In this manuscript we share our progress towards generation of a comprehensive kinase chemogenomic set (KCGS), release kinome profiling data of a large inhibitor set (Published Kinase Inhibitor Set 2 (PKIS2)), and outline a process through which the community can openly collaborate to create a KCGS that probes the full complement of human protein kinases.
Metadaten| Author: | David H. DrewryORCiD, Carrow I. WellsORCiD, David M. AndrewsORCiD, Richard Angell, Hassan Al-AliORCiD, Alison D. AxtmanORCiD, Stephen J. Capuzz, Jonathan M. ElkinsORCiD, Peter EttmayerORCiDGND, Mathias FrederiksenORCiD, Opher Gileadi, Nathanael S. GrayORCiDGND, Alice Hooper, Stefan KnappORCiD, Stefan Laufer, Ulrich Lücking, Michael Michaelides, Susanne Müller, Eugene Muratov, R. Aldrin Denny, Kumar S. Saikatendu, Daniel K. Treiber, William J. ZuercherORCiD, Timothy M. WillsonORCiD |
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| URN: | urn:nbn:de:hebis:30:3-439825 |
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| DOI: | https://doi.org/10.1371/journal.pone.0181585 |
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| ISSN: | 1932-6203 |
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| Pubmed Id: | https://pubmed.ncbi.nlm.nih.gov/28767711 |
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| Parent Title (English): | PLoS one |
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| Publisher: | PLoS |
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| Place of publication: | Lawrence, Kan. |
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| Contributor(s): | Anette Duensing |
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| Document Type: | Article |
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| Language: | English |
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| Date of Publication (online): | 2017/08/03 |
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| Date of first Publication: | 2017/08/02 |
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| Publishing Institution: | Universitätsbibliothek Johann Christian Senckenberg |
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| Release Date: | 2017/08/03 |
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| Volume: | 12 |
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| Issue: | (8): e0181585 |
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| Page Number: | 20 |
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| First Page: | 1 |
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| Last Page: | 20 |
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| Note: | Copyright: © 2017 Drewry et al. This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. |
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| HeBIS-PPN: | 416311369 |
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| Institutes: | Biochemie, Chemie und Pharmazie / Pharmazie |
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| Exzellenzcluster / Exzellenzcluster Makromolekulare Komplexe |
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| Dewey Decimal Classification: | 6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit |
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| Sammlungen: | Universitätspublikationen |
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| Licence (German): |  Creative Commons - Namensnennung 4.0 |
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Creative Commons - Namensnennung 4.0