Drewry, DH;
Wells, CI;
Andrews, DM;
Angell, R;
Al-Ali, H;
Axtman, AD;
Capuzzi, SJ;
... Willson, TM; + view all
(2017)
Progress towards a public chemogenomic set for protein kinases and a call for contributions.
PLOS ONE
, 12
(8)
, Article e0181585. 10.1371/journal.pone.0181585.
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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.
| Type: | Article |
|---|---|
| Title: | Progress towards a public chemogenomic set for protein kinases and a call for contributions |
| Open access status: | An open access version is available from UCL Discovery |
| DOI: | 10.1371/journal.pone.0181585 |
| Publisher version: | https://doi.org/10.1371/journal.pone.0181585 |
| Language: | English |
| Additional information: | This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/ |
| Keywords: | Science & Technology, Multidisciplinary Sciences, Science & Technology - Other Topics, CANCER-CELLS, INHIBITOR, IDENTIFICATION, INTERROGATION, SENSITIVITY, SELECTIVITY, DEPENDENCY, TARGETS |
| UCL classification: | UCL UCL > Provost and Vice Provost Offices > VP: Health UCL > Provost and Vice Provost Offices > VP: Health > Translational Research Office |
| URI: | https://discovery.ucl.ac.uk/id/eprint/10078246 |
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