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Team descubre estructuras moleculares claves para los coágulos sanguíneos
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News provided by

Shanghai Institute of Materia, CAS

Apr 30, 2014, 13:00 ET

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-- Las estructuras del receptor P2Y12 humano, claves para la próxima generación de fármacos antitrombóticos  

SHANGHAI, 30 de abril de 2014 /PRNewswire/ -- El equipo internacional dirigido por científicos del Shanghai Institute of Materia Medica, Chinese Academy of Sciences (SIMM) ha descubierto la estructura detallada de un receptor que desempeña un papel clave en la activación plaquetaria y coagulación sanguínea. El trabajo tiene implicaciones para el tratamiento de las enfermedades cardiovasculares y otras.  

En un par de documentos publicados por la revista Nature el 1 de mayo, los científicos ofrecen un mapa detallado de P2Y12R, un receptor de proteína combinada Gi humana. El objetivo de fármaco antitrombótico tiene un mercado de varios miles de millones de dólares estadounidenses.  

"Este nuevo trabajo no solo profundizará el conocimiento de la activación de esta súper familia de receptores, sino que también ofrecerá una inestimable visión de la mejora y desarrollo de fármacos P2Y12 orientados a las enfermedades cardiovasculares y otras", dijo el líder del equipo Qiang Zhao, profesor en SIMM. "Estuve particularmente orgulloso de la colaboración internacional de alta calidad entre China, EE. UU. y Alemania que llevó a completar esta investigación".

Las estructuras fueron solucionadas por SIMM en colaboración con los grupos de investigación del National Institutes of Health (NIH; Estados Unidos), The Scripps Research Institute GPCR Network (Estados Unidos), iHuman Institute of ShanghaiTech University (China) y la Universidad de Bonn (Alemania).

"Lo que hemos aprendido de esta investigación podría preparar el camino para la creación de fármacos con menos limitaciones y riesgos para la salud", dijo el doctor Kenneth A. Jacobson. "Nuestros descubrimientos tienen el potencial para marcar una importante diferencia en las vidas de los pacientes".

La activación inadecuada de las plaquetas puede resultar posteriormente en condiciones que ponen en peligro la vida con anginas inestables, ataque cardiaco y derrame. Cada uno de los fármacos P2Y12R comercializados actualmente tiene determinadas limitaciones, y los esfuerzos por desarrollar mejores fármacos han estado obstruidos por un escaso conocimiento de la interacción de receptores de ligando. 

Estos estudios describen por primera vez la estructura del P2Y12R, en complejo con un agonista complete y un antagonista reversible P2Y12R no nucleótido diseñado por AstraZeneca. Combinando el completo conocimiento obtenido de las tres estructuras, los investigadores consiguieron un conocimiento detallado de los diferentes tipos de fármacos por el receptor.  

"La investigación del receptor Th P2Y12 da esperanza para otras aplicaciones", indicó la doctora Christa E. Muller, de la University of Bonn. "Así, el receptor P2Y12 relacionado, por ejemplo, está implicado en la metástasis de las células tumorales. Además, también podrían surgir nuevas opciones para la investigación del cáncer".

SOURCE Shanghai Institute of Materia, CAS

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