Structural Basis of Swinholide A Binding to Actin
Copyright policy )Structural Basis of Swinholide A Binding to Actin
Marine toxins targeting the actin cytoskeleton represent a new and promising class of anti-cancer compounds. Here we present a 2.0 A resolution structure of swinholide A, a marine macrolide, bound to two actin molecules. The structure demonstrates that the actin dimer in the complex does not represent a physiologically relevant entity, for the two actin molecules do not interact with each other. The swinholide A actin binding site is the same as that targeted by toxins of the trisoxazole family and numerous actin binding proteins, highlighting the importance of this site in actin polymerization. The observed structure reveals the mechanism of action of swinholide A and provides a structural framework about which to design new agents directed at the cytoskeleton.
- University of Wisconsin System United States
- University of Wisconsin–Oshkosh United States
- University of Wisconsin–Madison United States
- University of the Ryukyus Japan
Pharmacology, Binding Sites, Clinical Biochemistry, Biochemistry, Actins, Structure-Activity Relationship, Drug Discovery, Molecular Medicine, Marine Toxins, Molecular Biology, Protein Binding
Pharmacology, Binding Sites, Clinical Biochemistry, Biochemistry, Actins, Structure-Activity Relationship, Drug Discovery, Molecular Medicine, Marine Toxins, Molecular Biology, Protein Binding
citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).69 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Top 10% influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 10% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Top 10%
Citations provided by BIP!Popularity provided by BIP!