Supramolecular alleviation of cardiotoxicity of a small-molecule kinase inhibitor

Abstract : Small-molecule kinase inhibitors (SMKIs) have been widely used in the treatment of a variety of cancers due to their clinically demonstrated efficacy. However, the use of some SMKIs, such as sorafenib (SO), has been plagued by their cardiotoxicity that has been frequently observed in treated patients. Herein we report that the encapsulation of SO by a synthetic receptor cucurbit[7]uril (CB[7]) alleviated the inherent cardiotoxicity of SO, as demonstrated in an in vivo zebrafish model. Moreover, the anti-cancer activity of SO was well preserved, upon its encapsulation by CB[7], as demonstrated by both in vitro and in vivo cancer/angiogenesis models. This discovery may provide new insights into a novel supramolecular formulation of SMKIs for the management of their side-effects.
Type de document :
Article dans une revue
Organic and Biomolecular Chemistry, Royal Society of Chemistry, 2017, 15 (38), pp.8046--8053. 〈10.1039/c7ob01505d〉
Domaine :
Liste complète des métadonnées

https://hal-amu.archives-ouvertes.fr/hal-01774176
Contributeur : Marlene Delhaye <>
Soumis le : lundi 23 avril 2018 - 14:41:15
Dernière modification le : mardi 3 juillet 2018 - 11:23:04

Identifiants

Collections

Citation

Xue Yang, Qiaoxian Huang, David Bardelang, Chunming Wang, Simon M. Y. Lee, et al.. Supramolecular alleviation of cardiotoxicity of a small-molecule kinase inhibitor. Organic and Biomolecular Chemistry, Royal Society of Chemistry, 2017, 15 (38), pp.8046--8053. 〈10.1039/c7ob01505d〉. 〈hal-01774176〉

Partager

Métriques

Consultations de la notice

43