Professeur Kazuma Yasuhara
Nara Institute of Science & Technology, Japan
"Biomimetic design of new generation antimicrobial agents by learning from nature - How to fight drug-resistant bacteria."
Abstract
Resistance of pathogens against antibiotics is now a serious public health issue in the world. There is an urgent need for the development of novel antimicrobial agents, which act through a different mechanism from conventional antibiotics.
In nature, there are antimicrobial peptides (AMPs), which show antimicrobial activity against a wide spectrum of bacteria without resistance development. AMPs attack cell membrane that contrasts specific protein-targeting conventional antibiotics. AMPs generally have several cationic amino acid residues to selectively recognize negatively charged bacterial membrane over neutral host cell membrane.
Additionally, AMPs form a facially amphiphilic structure in which cationic and hydrophobic amino acid residues are segregated in each face on a secondary structure of the peptide. We have developed synthetic AMP mimics by employing macrocyclic molecular frameworks. The AMP mimicking agents have amphiphilic nature originated in the cationic group as well as hydrophobic moieties. Bioactivity assay revealed that out antimicrobial agents express high antimicrobial activity. In addition, model membrane study using a fluorescent dye entrapping liposome.
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