Progress towards a public chemogenomic set for protein kinases and a call for contributions.
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 s...
Saved in:
| Main Authors: | , , , , , , , , , , , , , , , , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Public Library of Science (PLoS)
2017-01-01
|
| Series: | PLoS ONE |
| Online Access: | https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0181585&type=printable |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1850078966760603648 |
|---|---|
| author | David H Drewry Carrow I Wells David M Andrews Richard Angell Hassan Al-Ali Alison D Axtman Stephen J Capuzzi Jonathan M Elkins Peter Ettmayer Mathias Frederiksen Opher Gileadi Nathanael Gray Alice Hooper Stefan Knapp Stefan Laufer Ulrich Luecking Michael Michaelides Susanne Müller Eugene Muratov R Aldrin Denny Kumar S Saikatendu Daniel K Treiber William J Zuercher Timothy M Willson |
| author_facet | David H Drewry Carrow I Wells David M Andrews Richard Angell Hassan Al-Ali Alison D Axtman Stephen J Capuzzi Jonathan M Elkins Peter Ettmayer Mathias Frederiksen Opher Gileadi Nathanael Gray Alice Hooper Stefan Knapp Stefan Laufer Ulrich Luecking Michael Michaelides Susanne Müller Eugene Muratov R Aldrin Denny Kumar S Saikatendu Daniel K Treiber William J Zuercher Timothy M Willson |
| author_sort | David H Drewry |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-ca1842e46c3c4d9282fcf8bc425a50a8 |
| institution | DOAJ |
| issn | 1932-6203 |
| language | English |
| publishDate | 2017-01-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS ONE |
| spelling | doaj-art-ca1842e46c3c4d9282fcf8bc425a50a82025-08-20T02:45:24ZengPublic Library of Science (PLoS)PLoS ONE1932-62032017-01-01128e018158510.1371/journal.pone.0181585Progress towards a public chemogenomic set for protein kinases and a call for contributions.David H DrewryCarrow I WellsDavid M AndrewsRichard AngellHassan Al-AliAlison D AxtmanStephen J CapuzziJonathan M ElkinsPeter EttmayerMathias FrederiksenOpher GileadiNathanael GrayAlice HooperStefan KnappStefan LauferUlrich LueckingMichael MichaelidesSusanne MüllerEugene MuratovR Aldrin DennyKumar S SaikatenduDaniel K TreiberWilliam J ZuercherTimothy M WillsonProtein 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.https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0181585&type=printable |
| spellingShingle | David H Drewry Carrow I Wells David M Andrews Richard Angell Hassan Al-Ali Alison D Axtman Stephen J Capuzzi Jonathan M Elkins Peter Ettmayer Mathias Frederiksen Opher Gileadi Nathanael Gray Alice Hooper Stefan Knapp Stefan Laufer Ulrich Luecking Michael Michaelides Susanne Müller Eugene Muratov R Aldrin Denny Kumar S Saikatendu Daniel K Treiber William J Zuercher Timothy M Willson Progress towards a public chemogenomic set for protein kinases and a call for contributions. PLoS ONE |
| title | Progress towards a public chemogenomic set for protein kinases and a call for contributions. |
| title_full | Progress towards a public chemogenomic set for protein kinases and a call for contributions. |
| title_fullStr | Progress towards a public chemogenomic set for protein kinases and a call for contributions. |
| title_full_unstemmed | Progress towards a public chemogenomic set for protein kinases and a call for contributions. |
| title_short | Progress towards a public chemogenomic set for protein kinases and a call for contributions. |
| title_sort | progress towards a public chemogenomic set for protein kinases and a call for contributions |
| url | https://journals.plos.org/plosone/article/file?id=10.1371/journal.pone.0181585&type=printable |
| work_keys_str_mv | AT davidhdrewry progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT carrowiwells progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT davidmandrews progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT richardangell progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT hassanalali progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT alisondaxtman progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT stephenjcapuzzi progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT jonathanmelkins progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT peterettmayer progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT mathiasfrederiksen progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT ophergileadi progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT nathanaelgray progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT alicehooper progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT stefanknapp progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT stefanlaufer progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT ulrichluecking progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT michaelmichaelides progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT susannemuller progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT eugenemuratov progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT raldrindenny progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT kumarssaikatendu progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT danielktreiber progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT williamjzuercher progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions AT timothymwillson progresstowardsapublicchemogenomicsetforproteinkinasesandacallforcontributions |