Incorporation of β-Silicon-β3-Amino Acids in the Antimicrobial Peptide Alamethicin Provides a 20-Fold Increase in Membrane Permeabilization
作者:Julie L. H. Madsen、Claudia U. Hjørringgaard、Brian S. Vad、Daniel Otzen、Troels Skrydstrup
DOI:10.1002/chem.201600445
日期:2016.6.6
Incorporation of silicon‐containing amino acids in peptides is known to endow the peptide with desirable properties such as improved proteolytic stability and increased lipophilicity. In the presented study, we demonstrate that incorporation of β‐silicon‐β3‐amino acids into the antimicrobialpeptidealamethicinprovides the peptide with improved membranepermeabilizing properties. A robust synthetic
replacement of Trp3 by Phe3. Additionally, the totalsynthesis of 1 and 2 was accomplished by a solid-phase approach, confirming the absoluteconfiguration of all chiral amino acids as l. Both the chilenopeptins (1 and 2) and tylopeptins (3 and 4) were evaluated for their potential to inhibit the growth of phytopathogenic organisms.
Synthesis, Conformational Analysis and Antitumor Activity of the Naturally Occurring Antimicrobial Medium-Length Peptaibol Pentadecaibin and Spin-Labeled Analogs Thereof
作者:Laura Morbiato、Celeste Quaggia、Luca Menilli、Chiara Dalla Torre、Antonio Barbon、Marta De Zotti
DOI:10.3390/ijms241713396
日期:——
sequences, side reactions and difficult purification steps. Herein, we describe our strategy and itsapplication to the synthesis of spin-labeled analogs of the recently discovered, natural, medium-length peptaibol pentadecaibin. We studied the antitumor activity of pentadecaibin and its analogs, finding potent cytotoxicity against human triple-negative breast cancer and ovarian cancer. Finally, our analysis
[EN] PROCESS FOR PRODUCING DETERGENT MOLECULES COMPRISING AN ETHER LINKAGE FROM BUTADIENE<br/>[FR] PROCEDE DE PRODUCTION DE MOLECULES DETERGENTES A LIAISON ETHER A PARTIR DE BUTADIENE