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Fotomodulación del transporte y el potencial de la transmembrana por medio de bistioureas basadas en estilebeno

Sander J Wezenberg^1,2, Li-Jun Chen³, Jasper E Bos¹

¹Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.

Journal of the American Chemical Society

|December 21, 2021

Resumen

Los investigadores desarrollaron bis (tio) ureas sensibles a la luz para controlar el transporte transmembrana. Estas moléculas muestran una mayor unión y transporte de cloruro en su forma de isómero (Z), lo que permite la modulación del potencial de membrana fotocontrolada.

Área de la Ciencia:

Química supramolecular
Biología Química
Biofísica de las membranas

Sus antecedentes:

Las proteínas de transporte de membrana regulan las funciones biológicas y responden a los estímulos ambientales.
El desarrollo de receptores de moléculas pequeñas para el transporte transmembrana sensible a estímulos sigue siendo un desafío.

Objetivo del estudio:

Crear sistemas de transporte de transmembrana controlables por la luz utilizando nuevos derivados de bis (tio) urea.
Para investigar el fotocontrol del potencial de la membrana y el transporte de aniones.

Principales métodos:

Síntesis de bis (tio) ureas derivadas de los estilebenos rígidos.
Espectroscopia UV-vis y RMN de 1H para el seguimiento de la fotoisomerización E-Z.
Títulos de RMN de 1H, cristalografía de rayos X y cálculos de DFT para el análisis de la unión.
Ensayos de transporte de transmembrana para evaluar la actividad de los isómeros.

Principales resultados:

Las bis (tio) ureas se someten a una fotoisomerización E-Z reversible tras la irradiación UV.
El isómero (Z) exhibe una unión de cloruro significativamente más fuerte en comparación con el isómero (E).
Los isómeros (Z) demuestran una actividad sustancialmente mayor en la mediación del transporte transmembrana.
La irradiación de luz modula efectivamente tanto el transporte de la membrana como la despolarización de la membrana.

Conclusiones:

Se han desarrollado bis (tio) ureas con interruptor de luz que permiten el transporte de aniones fotocontrolados.
Estos hallazgos ofrecen potencial para terapias basadas en la luz y herramientas optofarmacológicas.
El sistema proporciona un nuevo enfoque para el estudio de las enfermedades asociadas al transporte de aniones y la actividad neuronal.

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