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La predicción de la escisión de la prohormona descubre un péptido antiobesidad sin incretina

Laetitia Coassolo^1,2,3, Niels B Danneskiold-Samsøe^1,2, Quennie Nguyen¹

¹Department of Pathology, Stanford University School of Medicine, Stanford, CA, USA.

|March 5, 2025

Resumen

Los investigadores descubrieron un nuevo péptido, BRP, que reduce la ingesta de alimentos y combate la obesidad en modelos animales. Este péptido, identificado mediante el descubrimiento computacional de fármacos, ofrece un nuevo terapéutico potencial para el control del peso sin efectos adversos.

Área de la Ciencia:

La bioquímica
Endocrinología
Farmacología

Sus antecedentes:

Las hormonas péptidas regulan el equilibrio energético.
La prohormona convertasa 1/3 (PCSK1) es crucial para el procesamiento de péptidos, incluidos los objetivos terapéuticos como el péptido similar al glucagón 1 (GLP-1).
La gama completa de péptidos generados por PCSK1 y sus funciones no se comprenden completamente.

Objetivo del estudio:

Mapear sistemáticamente los fragmentos de péptidos proteolíticos humanos no caracterizados anteriormente generados por las prohormonas convertidas.
Identificar nuevos péptidos bioactivos con aplicaciones terapéuticas potenciales.
Investigar los efectos y mecanismos contra la obesidad de un péptido recién identificado, BRP.

Principales métodos:

Se empleó el descubrimiento computacional de fármacos para mapear más de 2.600 fragmentos de péptidos proteolíticos humanos.
Se identificó un nuevo péptido de 12 meros, el péptido relacionado con BRINP2 (BRP).
La administración farmacológica de BRP en ratones y cerdos se utilizó para evaluar sus efectos sobre la ingesta de alimentos y el peso corporal.

Principales resultados:

Identificación de más de 2.600 fragmentos de péptidos no caracterizados anteriormente.
Descubrimiento y caracterización del péptido de 12 meros, BRP.
La administración de BRP redujo la ingesta de alimentos y demostró efectos antiobesidad en ratones y cerdos, sin náuseas ni aversión.
BRP desencadenó la activación central de FOS y actuó independientemente de la leptina, el receptor GLP- 1 y el receptor de la melanocortina 4.

Conclusiones:

Un nuevo método computacional permite la identificación de nuevos péptidos bioactivos.
BRP es un péptido validado farmacológicamente con potencial terapéutico para modular el peso corporal.
BRP representa una nueva vía prometedora para los tratamientos contra la obesidad.

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