Scaffold hopping from (5-hydroxymethyl) isophthalates to multisubstituted pyrimidines diminishes binding affinity to the C1 domain of protein kinase C.

Protein kinase C (PKC) isoforms play a pivotal role in the regulation of numerous cellular functions, making them extensively studied and highly attractive drug targets. Utilizing the crystal structure of the PKCδ C1B domain, we have developed hydrophobic isophthalic acid derivatives that modify PKC...

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Bibliographic Details
Main Authors: Riccardo Provenzani, Ilari Tarvainen, Giulia Brandoli, Antti Lempinen, Sanna Artes, Ainoleena Turku, Maria Helena Jäntti, Virpi Talman, Jari Yli-Kauhaluoma, Raimo K Tuominen, Gustav Boije Af Gennäs
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2018-01-01
Series:PLoS ONE
Online Access:http://europepmc.org/articles/PMC5895059?pdf=render