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Explotación de la alosteria humana de la fucosiltransferasa 8 con un inhibidor covalente para la supresión de la
Jiheng Jiang1,2, Dongyang He2, Mengyu Ke2
1Key Laboratory of Glyco-drug Research of Zhejiang Province, School of Chemistry and Materials Science, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou, China.
Nature communications
|February 10, 2026
Resumen
Los investigadores descubrieron un nuevo sitio alostérico en la fucosiltransferasa 8 (FUT8), lo que permite el desarrollo de CAIF, un nuevo inhibidor covalente. Este avance ofrece una estrategia prometedora para dirigirse a FUT8 en la terapia del cáncer.
Área de la Ciencia:
- La bioquímica es la bioquímica.
- Descubrimiento de Drogas Descubrimiento de Drogas
- Biología del cáncer Biología del cáncer.
Sus antecedentes:
- La fucosilación del núcleo, mediada por la fucosiltransferasa 8 (FUT8), es crucial en la progresión del cáncer, la evasión inmune y la resistencia a los medicamentos.
- El desarrollo de inhibidores selectivos de FUT8 es un desafío debido a la especificidad conservada del sustrato entre las fucosiltransferasas.
Objetivo del estudio:
- Identificar nuevos objetivos terapéuticos y desarrollar inhibidores selectivos para FUT8.
- Explorar estrategias de inhibición alostérica para dirigir la actividad de FUT8.
Principales métodos:
- Diseño de fármacos basado en la estructura utilizando cribado de alto rendimiento y estudios cristalográficos.
- Desarrollo de un inhibidor covalente, CAIF, dirigido a un sitio alostérico en FUT8.8.
- Ensayos celulares in vitro para evaluar la eficacia y la citotoxicidad del CAIF.
Principales resultados:
- Descubrimiento de un sitio alostérico no reconocido previamente en FUT8.8.
- CAIF, un nuevo inhibidor covalente, fue diseñado para atacar la lisina K216 dentro del sitio alostérico.
- CAIF demostró una citotoxicidad mínima, inhibió la fucosilación del núcleo y redujo la invasión de células cancerosas.
Conclusiones:
- CAIF representa un compuesto de plomo prometedor para las terapias contra el cáncer dirigidas a FUT8.
- Este estudio proporciona un marco novedoso para dirigirse a las glicosiltransferasas a través de la inhibición alostérica y covalente.
- Dirigirse al FUT8 alostéricamente ofrece una nueva vía para desarrollar inhibidores selectivos con toxicidad reducida.
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