The small-molecule BGP-15 protects against heart failure and atrial fibrillation in mice

Febbraio, MA; Mellet, NA; Woodcock, EA; Meikle, PJ; Tham, YK; Sapra, G; Du, XJ; Lim, L; Henstridge, DC; Sadoshima, J; Marasco, S; McMullen, JR; Bernardo, BC; Pretorius, L; Cemerlang, N; Boey, EJ; Ueyama, T; Matsumoto, A; Ooi, JY; Kiriazis, H
Abstract
Heart failure (HF) and atrial fibrillation (AF) share common risk factors, frequently coexist and are associated with high mortality. Treatment of HF with AF represents a major unmet need. Here we show that a small molecule, BGP-15, improves cardiac function and reduces arrhythmic episodes in two independent mouse models, which progressively develop HF and AF. In these models, BGP-15 treatment is associated with increased phosphorylation of the insulin-like growth factor 1 receptor (IGF1R), which is depressed in atrial tissue samples from patients with AF. Cardiac-specific IGF1R transgenic overexpression in mice with HF and AF recapitulates the protection observed with BGP-15. We further demonstrate that BGP-15 and IGF1R can provide protection independent of phosphoinositide 3-kinase-Akt and heat-shock protein 70; signalling mediators often defective in the aged and diseased heart. As BGP-15 is safe and well tolerated in humans, this study uncovers a potential therapeutic approach for HF and AF.
Journal NAT COMMUN
ISSN 2041-1723
Published 09 Dec 2014
Volume 5
Issue
Pages 5705
DOI 10.1038/ncomms6705
Type Journal Article
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