Journal article
Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer
- Abstract:
- Kinases are signalling proteins which have proven to be successful targets for the treatment of a variety of diseases, predominantly in cancers. However, only a small proportion of kinases (<20%) have been investigated for their therapeutic viability, likely due to the lack of available chemical tools across the kinome. In this work we describe initial efforts in the development of a selective chemical tool for protein kinase N2 (PKN2), a relatively unexplored kinase of interest in several types of cancer. The most successful compound, 5, has a measured IC<sub>50</sub> of 0.064 μM against PKN2, with ca. 17-fold selectivity over close homologue, PKN1.
- Publication status:
- Published
- Peer review status:
- Peer reviewed
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(Preview, Version of record, 1.4MB, Terms of use)
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- Publisher copy:
- 10.1016/j.bmcl.2020.127040
Authors
- Publisher:
- Elsevier
- Journal:
- Bioorganic and Medicinal Chemistry Letters More from this journal
- Volume:
- 30
- Issue:
- 8
- Article number:
- 127040
- Publication date:
- 2020-02-17
- Acceptance date:
- 2020-02-14
- DOI:
- EISSN:
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1464-3405
- ISSN:
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0960-894X
- Pmid:
-
32085971
- Language:
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English
- Keywords:
- Pubs id:
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1090287
- Local pid:
-
pubs:1090287
- Deposit date:
-
2021-10-28
Terms of use
- Copyright holder:
- Scott et al.
- Copyright date:
- 2020
- Rights statement:
- ©2020 The Authors. Published by Elsevier Ltd. This is an open access article under the CC BY license (http://creativecommons.org/licenses/BY/4.0/).
- Licence:
- CC Attribution (CC BY)
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