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Issue 5, 2017
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Site selective reading of epigenetic markers by a dual-mode synthetic receptor array

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Abstract

Variably functionalized self-folding deep cavitands form an arrayed, fluorescent indicator displacement assay system for the detection of post-translationally modified (PTM) histone peptides. The hosts bind trimethyllysine (KMe3) groups, and use secondary upper rim interactions to provide more sensitive discrimination between targets with identical KMe3 binding handles. The sensor array uses multiple different recognition modes to distinguish between miniscule differences in target, such as identical lysine modifications at different sites of histone peptides. In addition, the sensor is affected by global changes in structure, so it is capable of discriminating between identical PTMs, at identical positions on amino acid fragments that vary only in peptide backbone length, and can be applied to detect non-methylation modifications such as acetylation and phosphorylations located multiple residues away from the targeted binding site. The synergistic application of multiple variables allows dual-mode deep cavitands to approach levels of recognition selectivity usually only seen with antibodies.

Graphical abstract: Site selective reading of epigenetic markers by a dual-mode synthetic receptor array

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Publication details

The article was received on 23 Feb 2017, accepted on 21 Mar 2017 and first published on 22 Mar 2017


Article type: Edge Article
DOI: 10.1039/C7SC00865A
Citation: Chem. Sci., 2017,8, 3960-3970
  • Open access: Creative Commons BY license
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    Site selective reading of epigenetic markers by a dual-mode synthetic receptor array

    Y. Liu, L. Perez, M. Mettry, A. D. Gill, S. R. Byers, C. J. Easley, C. J. Bardeen, W. Zhong and R. J. Hooley, Chem. Sci., 2017, 8, 3960
    DOI: 10.1039/C7SC00865A

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