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Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer

Scott, Fiona, Fala, Angela M., Pennicott, Lewis E., Reuillon, Tristan D., Massirer, Katlin B., Elkins, Jonathan M. and Ward, Simon E. 2020. Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer. Bioorganic and Medicinal Chemistry Letters 30 (8) , 127040. 10.1016/j.bmcl.2020.127040

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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 IC50 of 0.064 μM against PKN2, with ca. 17-fold selectivity over close homologue, PKN1.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Advanced Research Computing @ Cardiff (ARCCA)
Medicine
MRC Centre for Neuropsychiatric Genetics and Genomics (CNGG)
Publisher: Elsevier
ISSN: 0960-894X
Date of First Compliant Deposit: 26 June 2020
Date of Acceptance: 14 February 2020
Last Modified: 29 Jun 2020 10:45
URI: http://orca-mwe.cf.ac.uk/id/eprint/132824

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