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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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Publication details

The article was received on 02 Apr 2017, accepted on 29 Aug 2017 and first published on 30 Aug 2017


Article type: Edge Article
DOI: 10.1039/C7SC01475A
Citation: Chem. Sci., 2017,8, 7604-7610
  • Open access: Creative Commons BY license
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    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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