Actualizaciones sobre la orientación terapéutica de la diguanilato ciclasa para el tratamiento de infecciones bacterianas: una revisión exhaustiva

Video Experimental Relacionado

Updated: Sep 10, 2025

Establishment of a High-throughput Setup for Screening Small Molecules That Modulate c-di-GMP Signaling in Pseudomonas aeruginosa

Establishment of a High-throughput Setup for Screening Small Molecules That Modulate c-di-GMP Signaling in Pseudomonas aeruginosa

Published on: June 30, 2016

Roshan Mukund Tawale¹, Rafwana Ibrahim¹, Jesil Mathew Aranjani²

¹Department of Pharmaceutical Biotechnology, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, 576104, Manipal, India.

World journal of microbiology & biotechnology

|August 26, 2025

Resumen

La resistencia a los antimicrobianos requiere nuevos tratamientos. Dirigirse a las enzimas diguanilato ciclasa (DGC), cruciales para la virulencia bacteriana y la formación de biopelículas, ofrece una estrategia prometedora para el desarrollo de nuevos antibióticos y terapias combinadas.

Área de la Ciencia:

Microbiología
La bioquímica
Descubrimiento de drogas

Sus antecedentes:

La resistencia a los antimicrobianos (AMR) es una gran amenaza para la salud mundial que exige nuevos enfoques terapéuticos.
Las ciclases de diguanilato multisubunitaria (DGC) son reguladores clave de la virulencia bacteriana, controlando la formación de biopelículas, la motilidad y la patogénesis.
Los DGCs sintetizan di-GMP cíclico (c-di-GMP), un segundo mensajero crítico en las bacterias.

Objetivo del estudio:

Revisar los aspectos estructurales y funcionales de las DGC.
Para explorar el papel de los DGC en la patogénesis bacteriana.
Para resumir los avances recientes en las terapias dirigidas a DGC.

Principales métodos:

Revisión de la literatura centrada en la biología estructural, la química medicinal y la administración de medicamentos.
Análisis de los inhibidores de DGC, incluidas las moléculas pequeñas y los péptidos.
Examen de las terapias combinadas que incluyen inhibidores de la DGC.

Principales resultados:

Los DGC son objetivos validados para combatir las infecciones bacterianas.
Las innovaciones incluyen nuevas terapias de pequeñas moléculas y péptidos, y sistemas avanzados de administración de medicamentos.
Las terapias combinadas con inhibidores de DGC y antibióticos convencionales muestran potencial.

Conclusiones:

Dirigirse a los DGC presenta importantes oportunidades para desarrollar nuevas estrategias antimicrobianas.
Los avances en biología estructural y química medicinal están acelerando el desarrollo de fármacos para los inhibidores de DGC.
La traducción clínica de terapias dirigidas a DGC requiere abordar los desafíos existentes y explorar nuevas perspectivas.

Palabras clave:

Resistencia a los antimicrobianos Antivirulencia y sus derivados Infecciones bacterianas Las biofilmas C-di-GMP y sus derivados Diguanilato ciclasa y sus derivados Inhibidores de las moléculas pequeñas

Más Videos Relacionados

Capture Compound Mass Spectrometry - A Powerful Tool to Identify Novel c-di-GMP Effector Proteins

Capture Compound Mass Spectrometry - A Powerful Tool to Identify Novel c-di-GMP Effector Proteins

Published on: March 29, 2015

Identifying the Binding Proteins of Small Ligands with the Differential Radial Capillary Action of Ligand Assay DRaCALA

Identifying the Binding Proteins of Small Ligands with the Differential Radial Capillary Action of Ligand Assay DRaCALA

Published on: March 19, 2021

Videos de Conceptos Relacionados

GPCRs Regulate Adenylyl Cylase Activity

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...

G Protein-coupled Receptors

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...

Transducer Mechanism: Enzyme-Linked Receptors

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:

Targets for Drug Action: Overview

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...

Activation and Inactivation of G Proteins

Activation and Inactivation of G Proteins

Heterotrimeric G proteins are guanine nucleotide-binding proteins. As the name suggests, heterotrimeric G proteins are composed of three subunits: alpha, beta, and gamma. They remain GDP-bound or GTP-bound inside the cells and switch between inactive/active states. The Gα subunit possesses the nucleotide-binding pocket that binds guanine nucleotides and switches between GDP or GTP-bound states. In contrast, the Gꞵ and Gγ subunits are always bound together with high...

Gene Regulation in Microbial Communities: Quorum Sensing

Gene Regulation in Microbial Communities: Quorum Sensing

Quorum sensing is a mechanism of bacterial communication that enables coordinated gene expression in response to changes in population density. This facilitates collective behaviors that enhance survival, resource acquisition, and ecological adaptation. This process relies on small signaling molecules called autoinducers that accumulate as bacterial populations grow. When a critical threshold concentration of autoinducers is reached, bacterial cells collectively modify gene expression,...