Progress towards a public chemogenomic set for protein kinases and a call for contributions
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Drewry, David H, et al. Progress Towards a Public Chemogenomic Set for Protein Kinases and a Call for Contributions. 2017. https://doi.org/10.17615/7aj6-5547APA
Drewry, D., Wells, C., Andrews, D., Angell, R., Al Ali, H., Axtman, A., Capuzzi, S., Elkins, J., Ettmayer, P., Frederiksen, M., Gileadi, O., Gray, N., Hooper, A., Knapp, S., Laufer, S., Luecking, U., Michaelides, M., Müller, S., Muratov, E., Denny, R., Saikatendu, K., Treiber, D., Zuercher, W., & Willson, T. (2017). Progress towards a public chemogenomic set for protein kinases and a call for contributions. https://doi.org/10.17615/7aj6-5547Chicago
Drewry, David H., Carrow I Wells, David M Andrews, Richard Angell, Hassan Al Ali, Alison D Axtman, Stephen J Capuzzi et al. 2017. Progress Towards a Public Chemogenomic Set for Protein Kinases and a Call for Contributions. https://doi.org/10.17615/7aj6-5547- Creator
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Drewry, David H.
- Affiliation: Eshelman School of Pharmacy
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Wells, Carrow I.
- Affiliation: Eshelman School of Pharmacy
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Andrews, David M.
- Other Affiliation: AstraZeneca
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Angell, Richard
- Other Affiliation: Drug Discovery Group; University College London School of Pharmacy
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Al-Ali, Hassan
- Other Affiliation: Peggy and Harold Katz Family Drug Discovery Center; University of Miami Miller School of Medicine
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Axtman, Alison D.
- Affiliation: Eshelman School of Pharmacy
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Capuzzi, Stephen J.
- Affiliation: Eshelman School of Pharmacy
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Elkins, Jonathan M.
- Other Affiliation: Structural Genomics Consortium; Universidade Estadual de Campinas—UNICAMP
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Ettmayer, Peter
- Other Affiliation: Boehringer Ingelheim RCV GmbH and Co. KG
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Frederiksen, Mathias
- Other Affiliation: Novartis Institutes for BioMedical Research; Novartis Campus
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Gileadi, Opher
- Other Affiliation: Structural Genomics Consortium; Target Discovery Institute; Nuffield Department of Clinical Medicine; University of Oxford
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Gray, Nathanael
- Other Affiliation: Harvard Department of Biological Chemistry and Molecular Pharmacology; Harvard Medical School
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Hooper, Alice
- Other Affiliation: Drug Discovery Group; University College London School of Pharmacy
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Knapp, Stefan
- Other Affiliation: Structural Genomics Consortium; Buchmann Institute for Molecular Life Sciences; Institute of Pharmaceutical Chemistry; Goethe University Frankfurt
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Laufer, Stefan
- Other Affiliation: Department of Pharmaceutical Chemistry; Institute of Pharmaceutical Sciences; Eberhard Karls Universität Tübingen
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Luecking, Ulrich
- Other Affiliation: Bayer Pharma AG; Drug Discovery
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Michaelides, Michael
- Other Affiliation: Oncology Chemistry; AbbVie
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Müller, Susanne
- Other Affiliation: Structural Genomics Consortium; Buchmann Institute for Molecular Life Sciences; Institute of Pharmaceutical Chemistry; Goethe University Frankfurt
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Muratov, Eugene
- Affiliation: Eshelman School of Pharmacy
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Denny, R. Aldrin
- Other Affiliation: Worldwide Medicinal Chemistry; Pfizer Inc.
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Saikatendu, Kumar S.
- Other Affiliation: Global Research Externalization; Takeda California; Inc.
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Treiber, Daniel K.
- Other Affiliation: DiscoverX Corporation
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Zuercher, William J.
- Affiliation: Eshelman School of Pharmacy
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Willson, Timothy M.
- Affiliation: Eshelman School of Pharmacy
- Abstract
- 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.
- Date of publication
- 2017
- Keyword
- Consortia
- Biology and Life Sciences
- Enzymology
- Commerce
- Entropy
- Chemical Compounds
- Enzyme Inhibitors
- Social Sciences
- Thermodynamics
- Medicine and Health Sciences
- Physics
- Small Molecules
- Kinase Inhibitors
- Enzymes
- Economics
- Sociology
- Biotechnology
- Organic Compounds
- Chemistry
- Physical Sciences
- Proteins
- Organic Chemistry
- Vendors
- Protein Kinases
- Pharmacology
- Biochemistry
- DOI
- Identifier
- PMCID: PMC5540273
- Publisher DOI: https://doi.org/10.1371/journal.pone.0181585
- PMID: 28767711
- Onescience id: f207222afe7d1a993dc4a4138ea389ffd83f9ebc
- Resource type
- Article
- Rights statement
- In Copyright
- Journal title
- PloS One
- Journal volume
- 12
- Journal issue
- 8
- Page start
- e0181585
- Language
- English
- ISSN
- 1932-6203
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