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Identificación rápida de agonistas selectivos de subtipo del receptor de somatostatina a través de la química

S P Rohrer¹, E T Birzin, R T Mosley

¹Department of Cell Biochemistry and Physiology, Merck Research Laboratories, Post Office Box 2000, Rahway, NJ 07065, USA. susanvrohrer@merck.com

Science (New York, N.Y.)

|October 23, 1998

Resumen

Los investigadores desarrollaron agonistas no peptídicos para los receptores de somatostatina, revelando las funciones de los receptores de somatostatina de subtipo 2 y -5 en la regulación de la liberación de glucagón, insulina y hormona del crecimiento.

Área de la Ciencia:

Endocrinología y Farmacología Molecular.
Gastroenterología y metabolismo.

Sus antecedentes:

Los receptores de somatostatina (SSTR) son cruciales en la regulación de varios procesos fisiológicos.
Comprender las funciones específicas de cada subtipo de SSTR es esencial para el desarrollo terapéutico.

Objetivo del estudio:

Identificar y caracterizar los agonistas no peptídicos para los cinco subtipos de receptores de somatostatina.
Para dilucidar las funciones fisiológicas mediadas por subtipos específicos de receptores de somatostatina.

Principales métodos:

Las bibliotecas combinatorias fueron sintetizadas basadas en el modelado molecular de agonistas de péptidos conocidos.
Los experimentos in vitro se llevaron a cabo utilizando agonistas no peptídicos selectivos para evaluar la función del receptor.

Principales resultados:

Se demostró que el receptor de somatostatina subtipo 2 (SSTR2) inhibe la liberación de glucagón de las células alfa pancreáticas.
El receptor de somatostatina de subtipo 5 (SSTR5) fue identificado como un mediador de la secreción de insulina de las células beta pancreáticas.
Se descubrió que tanto SSTR2 como SSTR5 regulan la liberación de la hormona del crecimiento de la glándula pituitaria anterior de la rata.

Conclusiones:

Los agonistas no peptídicos selectivos para los receptores de somatostatina proporcionan una poderosa herramienta para diseccionar sus funciones fisiológicas.
Estos hallazgos ponen de relieve las distintas funciones de SSTR2 y SSTR5 en la homeostasis de la glucosa y la regulación hormonal.

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