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Issue 30, 2016
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Structure–property relationships of photoresponsive inhibitors of the kinesin motor

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Abstract

Recently we demonstrated the photoregulation of the activity of kinesin-1 using an azobenzene-tethered peptide (azo-peptide: Azo-Ile-Pro-Lys-Ala-Ile-Gln-Ala-Ser-His-Gly-Arg-OH). To understand the mechanism behind this photoswitchable inhibition, here we studied the structure–property relationships of a range of azo-peptides through systematic variations in the structures of the peptide and azobenzene units. The vital peptide sequence for kinesin inhibition—mediated through electrostatic, hydrophobic and C–Hπ interactions—was the same as that for the self-inhibition of kinesin. We also identified substituents on the azobenzene capable of enhancing the photoswitchability of inhibition. As a result, we developed a new inhibitor featuring a relatively short peptide unit (-Arg-Ile-Pro-Lys-Ala-Ile-Arg-OH) and an azobenzene unit bearing a para-OMe group. In the trans form of its azobenzene unit, this finely tuned inhibitor stopped the kinesin-driven gliding motility of microtubules completely at a relatively low concentration, yet allowed gliding motility with a relatively high velocity in the cis form obtained after UV irradiation.

Graphical abstract: Structure–property relationships of photoresponsive inhibitors of the kinesin motor

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Publication details

The article was received on 02 May 2016, accepted on 27 May 2016 and first published on 31 May 2016


Article type: Paper
DOI: 10.1039/C6OB00951D
Citation: Org. Biomol. Chem., 2016,14, 7202-7210
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    Structure–property relationships of photoresponsive inhibitors of the kinesin motor

    A. S. Amrutha, K. R. S. Kumar, K. Matsuo and N. Tamaoki, Org. Biomol. Chem., 2016, 14, 7202
    DOI: 10.1039/C6OB00951D

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