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Exploración del DPP-4: implicaciones en diversas enfermedades y conocimientos estructurales para el diseño de nuevos

Ritam Dutta¹, Samima Khatun², Payel Ghosh¹

¹Department of Pharmaceutical Technology, JIS University, 81, Nilgunj Road, Agarpara, Kolkata 700109, West Bengal, India.

Bioorganic chemistry

|September 6, 2025

Resumen

La enzima dipeptidil peptidasa-4 (DPP-4) tiene un impacto más que la diabetes, afectando la inmunidad, la salud del corazón y el cáncer. Comprender su estructura ayuda en el desarrollo de nuevos inhibidores de la DPP-4 (DPP-4Is) para aplicaciones terapéuticas más amplias.

Área de la Ciencia:

Enzimología y Biología Molecular
Farmacología y descubrimiento de fármacos

Sus antecedentes:

La dipeptidil peptidasa-4 (DPP-4) es crucial en el metabolismo de la glucosa y en el tratamiento de la diabetes mellitus tipo 2 (DMT2) a través de gliptinas.
La investigación emergente revela papeles significativos de DPP-4 en la regulación inmune, las enfermedades cardiovasculares, el cáncer y la inflamación.

Objetivo del estudio:

Revisar las diversas funciones fisiológicas y patológicas de la DPP-4 más allá de la DM2.
Aclarar la base estructural de la inhibición de DPP-4 para el desarrollo terapéutico de próxima generación.

Principales métodos:

Revisión de la literatura existente sobre las funciones de la DPP-4 y el diseño del inhibidor.
Análisis de los datos estructurales de la cristalografía de rayos X y el modelado molecular.
Exploración del espacio químico para el desarrollo de un nuevo inhibidor de la DPP-4 (DPP-4I).

Principales resultados:

DPP-4 influye en numerosos péptidos bioactivos a través de la escisión del dipeptídeo N-terminal.
Los conocimientos estructurales revelan interacciones de unión clave y cambios conformacionales relevantes para el diseño del inhibidor.
La exploración del espacio químico ofrece un marco para el diseño racional del DPP-4I.

Conclusiones:

DPP-4 es un objetivo terapéutico versátil con implicaciones más allá de la DM2.
La comprensión de las relaciones estructura-actividad del DPP-4 es clave para desarrollar DPP-4Is avanzados.
La orientación de DPP-4 ofrece potencial para el tratamiento de una serie de enfermedades inflamatorias y metabólicas.

Palabras clave:

Espacio químico El DPP-4 Inhibidores de la DPP-4 Diabetes y otras enfermedades Relación entre estructura y actividad

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