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Issue 11, 2017
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Optical control of GPR40 signalling in pancreatic β-cells

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Abstract

Fatty acids activate GPR40 and K+ channels to modulate β-cell function. Herein, we describe the design and synthesis of FAAzo-10, a light-controllable GPR40 agonist based on Gw-9508. FAAzo-10 is a potent GPR40 agonist in the trans-configuration and can be inactivated on isomerization to cis with UV-A light. Irradiation with blue light reverses this effect, allowing FAAzo-10 activity to be cycled ON and OFF with a high degree of spatiotemporal precision. In dissociated primary mouse β-cells, FAAzo-10 also inactivates voltage-activated and ATP-sensitive K+ channels, and allows us to control glucose-stimulated Ca2+ oscillations in whole islets with light. As such, FAAzo-10 is a useful tool to study the complex effects, with high specificity, which FA-derivatives such as Gw-9508 exert at multiple targets in mouse β-cells.

Graphical abstract: Optical control of GPR40 signalling in pancreatic β-cells

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Supplementary files

Article information


Submitted
02 Apr 2017
Accepted
29 Aug 2017
First published
30 Aug 2017

This article is Open Access
All publication charges for this article have been paid for by the Royal Society of Chemistry

Chem. Sci., 2017,8, 7604-7610
Article type
Edge Article

Optical control of GPR40 signalling in pancreatic β-cells

J. A. Frank, D. A. Yushchenko, N. H. F. Fine, M. Duca, M. Citir, J. Broichhagen, D. J. Hodson, C. Schultz and D. Trauner, Chem. Sci., 2017, 8, 7604
DOI: 10.1039/C7SC01475A

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