Synthesis of kanamycin-peptide conjugates with antimicrobial activity.

• Grant number: 24/22341-9
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: July 01, 2025
• End date: June 30, 2026
• Field of knowledge: Biological Sciences - Microbiology - Applied Microbiology
• Principal Investigator: Eduardo Maffud Cilli
• Grantee: João Pedro Guimarães Nogueira
• Host Institution: Instituto de Química (IQ). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil

Abstract

The increasing bacterial resistance to existing antibiotics demands the development of new therapeutic strategies. Bacteria that inhabit the interior of mammalian cells represent a particularly challenging target, as they are protected from traditional drugs. The search for new molecules capable of penetrating infected cells and eliminating intracellular bacteria is essential for controlling resistant infections.In this context, cell-penetrating peptides (CPPs) emerge as promising alternatives to overcome these limitations. This project proposes the synthesis of new bioconjugates between kanamycin, an aminoglycoside-class antibiotic, and the HIV-TAT peptide (CPP). HIV-TAT facilitates the translocation of macromolecules across cell membranes, with the potential to evade bacterial efflux mechanisms.The conjugation of this peptide with kanamycin aims to enhance its antimicrobial efficacy against intracellular bacteria, reducing susceptibility to bacterial resistance and increasing penetration into phagocytic cells. Thus, the project seeks to develop more selective and effective antimicrobial compounds, contributing to new therapeutic approaches against resistant and persistent infections. (AU)