Inhibition of protein kinase C by synthetic xanthone derivatives

• 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: Bioorganic and Medicinal Chemistry

Vol. 11

Pages: 1215-1225

ISSN: 0968-0896

Publisher: Elsevier

Indexing

ISI Proceedings

ISI Web of Knowledge - 41 Citations

Scopus - 41 Citations

Scientific classification

FOS: Natural sciences > Chemical sciences

Other information

Authenticus ID: P-000-H39

DOI: 10.1016/s0968-0896(02)00641-7

Abstract (EN): The modulatory activity of two xanthones (3,4-dihydroxyxanthone and 1-formyl-4-hydroxy-3-methoxyxanthone) on isoforms alpha, betaI, delta, eta and zeta of protein kinase C (PKC) was evaluated using an in vivo yeast phenotypic assay. Both xanthones caused an effect compatible with PKC inhibition, similar to that elicited by known PKC inhibitors (chelerythrine and NPC 15437). PKC inhibition caused by xanthones was confirmed using an in vitro kinase assay. The yeast phenotypic assay revealed that xanthones present differences on their potency towards the distinct PKC isoforms tested. It is concluded that 3,4-dihydroxyxanthone and 1-formyl-4-hydroxy-3-methoxyxanthone may become useful PKC inhibitors and xanthone derivatives can be explored to develop new isoform-selective PKC inhibitors.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 11