We are pleased to announce that a paper titled “Antibacterial Metallacarborane-Peptide Hybrids Target the Membrane Potential in a Nonlytic Mode and Are Resistant to Proteolysis” has been published in the Journal of Medicinal Chemistry (200 points MNiSW, IF 6.8). Co-authors of the paper are Krzysztof Fink, PhD, Bożena Szermer-Olearnik, PhD, Michalina Gos, MA, and Tomasz Goszczyński, PhD, DSc from the Laboratory of Biomedical Chemistry, Mateusz Psurski, PhD Eng, from the Laboratory of Experimental Anticancer Therapy, and Paweł Migdal, PhD Eng, from the Interdepartmental Laboratory of Instrumental Analysis and Preparation.
This paper presents a new class of antimicrobial compounds – hybrids of peptides with metallocarboranes. This combination provides broad activity against Gram-positive and Gram-negative bacteria, with limited toxicity against mammalian cells. The mechanism of action of the compounds is based on depolarization of the bacterial cell membrane without its lysis, which leads to disruption of cellular homeostasis, a decrease in ATP levels, an increase in the production of reactive oxygen species and morphological changes in cells. A particularly important finding is that metallocarborane modification protects the peptide from trypsin digestion.
The work is the result of an international collaboration between researchers from Poland and the Czech Republic and was funded by the SONATINA project of the National Science Center (2019/32/C/NZ7/00510).
This is the fourth paper by employees of the Laboratory of Biomedical Chemistry to be published in the Journal of Medicinal Chemistry in the last four years.
Link to publication: