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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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Detalles Bibliográficos
Autores principales: Provenzani, Riccardo, Tarvainen, Ilari, Brandoli, Giulia, Lempinen, Antti, Artes, Sanna, Turku, Ainoleena, Jäntti, Maria Helena, Talman, Virpi, Yli-Kauhaluoma, Jari, Tuominen, Raimo K., Boije af Gennäs, Gustav
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5895059/
https://www.ncbi.nlm.nih.gov/pubmed/29641588
http://dx.doi.org/10.1371/journal.pone.0195668