Inhibition of alpha, beta I, delta, eta and zeta protein kinase C isoforms by xanthonolignoids

• Type: Article in International Scientific Journal
• Date: 2003

Authors

Saraiva, L (Author) FFUP; Fresco, P (Author) FFUP; Pinto, E (Author) FFUP; Sousa, E (Author) Other; Pinto, M (Author) FFUP; Goncalves, J (Author) FFUP

Journal

Title: Journal of Enzyme Inhibition and Medicinal Chemistry

Vol. 18

Pages: 357-370

ISSN: 1475-6366

Publisher: Taylor & Francis

Indexing

ISI Proceedings

ISI Web of Knowledge - 23 Citations

Scopus - 24 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-000-G40

DOI: 10.1080/147563601000118400

Abstract (EN): The effect of the xanthonolignoids trans -(+/-)-kielcorin C, cis -(+/-)-kielcorin C, trans -(+/-)-kielcorin D, trans -(+/-)-isokielcorin D and trans -(+/-)-kielcorin E on isoforms alpha, betaI, delta, eta and zeta of protein kinase C (PKC) was studied using the yeast phenotypic assay. All the compounds tested revealed an effect compatible with PKC inhibition, similar to that exhibited by the well established PKC inhibitor chelerythrine, and with differences in their potency towards the distinct isoforms tested, being, in general, potent inhibitors of the atypical PKC isoform (PKC-zeta). PKC inhibition caused by these kielcorins was confirmed using an in vitro kinase assay. The present study constitutes the first attempt to unravel the molecular mechanism of kielcorins activity, and shows that xanthonolignoids are a promising group of compounds to investigate for isoform selective PKC inhibitors.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 14