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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.

Original publication

DOI

10.1016/j.bmcl.2020.127040

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

15/04/2020

Volume

30

Keywords

AGC kinase, Benzimidazole, Cancer, Chemical probe, Chemical tool, Heart failure, Inflammation, Kinases, PKN2, PRK2, Protein kinase N2, Antineoplastic Agents, Benzimidazoles, Crystallography, X-Ray, Dose-Response Relationship, Drug, Drug Development, Humans, Models, Molecular, Molecular Structure, Neoplasms, Protein Kinase C, Protein Kinase Inhibitors, Structure-Activity Relationship