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El ácido retinoico 9-cis es un ligando de alta afinidad para el receptor retinoide X

R A Heyman¹, D J Mangelsdorf, J A Dyck

¹Ligand Pharmaceuticals, Inc., San Diego, California 92121.

|January 24, 1992

Resumen

Los investigadores descubrieron el ácido 9-cis retinoico (RA) como un potente ligando para el receptor retinoide X (RXR). Esta nueva hormona, que se encuentra en los organismos vivos, destaca la importancia del metabolismo de los retinoides en la señalización.

Área de la Ciencia:

Biología Molecular Biología Molecular
Endocrinología Endocrinología.
La bioquímica es la bioquímica.

Sus antecedentes:

El ácido retinoico all-trans (RA) modula la actividad del receptor del ácido retinoico (RAR) y del receptor del retinoide X (RXR).
La incapacidad de toda la AR trans para unirse a RXR sugiere un potencial metabolito con mayor afinidad.

Objetivo del estudio:

Para identificar el ligando RXR de alta afinidad sugerido por observaciones anteriores.
Investigar el papel del metabolismo de los retinoides en la generación de nuevas moléculas de señalización.

Principales métodos:

Enfoque experimental para identificar los ligandos RXR.
Pruebas de transfección para determinar la potencia del ligando.
Ensayos de unión de alta afinidad.
El cultivo celular y el análisis de tejidos (hígado, riñón) para detectar 9-cis RA.

Principales resultados:

Identificó 9-cis RA como un ligando de alta afinidad para RXR.
La AR con 9-cis demostró hasta 40 veces mayor potencia que la AR totalmente trans en ensayos de transfección.
Confirmó la producción endógena y la presencia de 9-cis RA en células cultivadas, hígado y riñón.

Conclusiones:

9-cis RA es una nueva hormona biológicamente activa que se une a RXR con alta afinidad.
El metabolismo de los retinoides juega un papel crucial en la generación de nuevas vías de señalización a través de la producción de nuevas hormonas.
El descubrimiento abre nuevas vías para comprender la señalización de los retinoides y su potencial terapéutico.

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