Počet záznamů: 1  

Optical control of GPR40 signalling in pancreatic beta-cells

  1. 1.
    0481801 - ÚOCHB 2018 RIV GB eng J - Článek v odborném periodiku
    Frank, J. A. - Yushchenko, Dmytro A. - Fine, N. H. F. - Duca, M. - Citir, M. - Broichhagen, J. - Hodson, D. J. - Schultz, C. - Trauner, D.
    Optical control of GPR40 signalling in pancreatic beta-cells.
    Chemical Science. Roč. 8, č. 11 (2017), s. 7604-7610. ISSN 2041-6520. E-ISSN 2041-6539
    Institucionální podpora: RVO:61388963
    Klíčová slova: protein-coupled receptor * insulin secretion * arachidonic acid
    Obor OECD: Biochemistry and molecular biology
    Impakt faktor: 9.063, rok: 2017
    http://pubs.rsc.org/en/content/articlehtml/2017/sc/c7sc01475a

    Fatty acids activate GPR40 and K+ channels to modulate beta-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 beta-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 beta-cells.
    Trvalý link: http://hdl.handle.net/11104/0277454

     
     
Počet záznamů: 1  

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