Issue 12, 2015

Synthetic aminopyrrolic receptors have apoptosis inducing activity

Abstract

We report two synthetic aminopyrrolic compounds that induce apoptotic cell death. These compounds have been previously shown to act as receptors for mannosides. The extent of receptor-induced cell death is greater in cells expressing a high level of high-mannose oligosaccharides than in cells producing lower levels of high-mannose glycans. The ability of synthetic receptors to induce cell death is attenuated in the presence of external mannosides. The present results provide support for the suggestion that the observed cell death reflects an ability of the receptors to bind mannose displayed on the cell surface. Signaling pathway studies indicate that the synthetic receptors of the present study promote JNK activation, induce Bax translocation to the mitochondria, and cause cytochrome c release from the mitochondria into the cytosol, thus promoting caspase-dependent apoptosis. Such effects are also observed in cells treated with mannose-binding ConA. The present results thus serve to highlight what may be an attractive new approach to triggering apoptosis via modes of action that differ from those normally used to promote apoptosis.

Graphical abstract: Synthetic aminopyrrolic receptors have apoptosis inducing activity

Supplementary files

Article information

Article type
Edge Article
Submitted
27 Aug 2015
Accepted
25 Sep 2015
First published
02 Oct 2015
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY-NC license

Chem. Sci., 2015,6, 7284-7292

Synthetic aminopyrrolic receptors have apoptosis inducing activity

S. Park, Y. P. Choi, J. Park, A. Share, O. Francesconi, C. Nativi, W. Namkung, J. L. Sessler, S. Roelens and I. Shin, Chem. Sci., 2015, 6, 7284 DOI: 10.1039/C5SC03200H

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