Intercalative DNA binding of the marine anticancer drug variolin B.

Abstract

Variolin B is a rare marine alkaloid that showed promising anti-cancer activity soon after its isolation. It acts as a cyclin-dependent kinase inhibitor, although the precise mechanism through which it exerts the cytotoxic effects is still unknown. The crystal structure of a variolin B bound to a DNA forming a pseudo-Holliday junction shows that this compound can also contribute, through intercalative binding, to either the formation or stabilization of multi-stranded DNA forms.

• Authors: Albert Canals, Raquel Arribas-Bosacoma, Fernando Albericio, Mercedes Álvarez, Joan Aymamí, Miquel Coll
• Journal: Scientific reports (Sci Rep) Vol. 7 Pg. 39680 (01 04 2017) ISSN: 2045-2322 [Electronic] England
• PMID: 28051169 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Aza Compounds
• Intercalating Agents
• Pyrimidines
• variolin B
• DNA

Topics

• Antineoplastic Agents (chemistry)
• Aza Compounds (chemistry)
• Crystallography, X-Ray
• DNA (chemistry)
• Intercalating Agents (chemistry)
• Models, Molecular
• Pyrimidines (chemistry)
• Structure-Activity Relationship