On November 1, 2017, Kumar, Prashant; Takayesu, Allen; Abbasi, Usama; Kalathottukaren, Manu Thomas; Abbina, Srinivas; Kizhakkedathu, Jayachandran N.; Straus, Suzana K. published an article.Category: amides-buliding-blocks The title of the article was Antimicrobial peptide-polymer conjugates with high activity: Influence of polymer molecular weight and peptide sequence on antimicrobial activity, proteolysis, and biocompatibility. And the article contained the following:
We report the synthesis, characterization, activity, and biocompatibility of a novel series of antimicrobial peptide-polymer conjugates. Using parent peptide aurein 2.2, we designed a peptide array (∼100 peptides) with single and multiple W and R mutations and identified antimicrobial peptides (AMPs) with potent activity against Staphylococcus aureus (S. aureus). These novel AMPs were conjugated to hyperbranched polyglycerols (HPGs) of different mol. weights and number of peptides to improve their antimicrobial activity and toxicity. The cell and blood compatibility studies of these conjugates demonstrated better properties than those of the AMP alone. However, conjugates showed lower antimicrobial activity in comparison to that of peptides, as determined from minimal inhibition concentrations (MICs) against S. aureus, but considerably better than that of the available polymer-AMP conjugates in the literature. In addition to measuring MICs and characterizing the biocompatibility, CD spectroscopy was used to investigate the interaction of the novel conjugates with model bacterial biomembranes. Moreover, the novel conjugates were exposed to trypsin to evaluate their stability. It was found that the conjugates resist proteolysis in comparison with unprotected peptides. The peptide conjugates were active in serum and whole blood. Overall, the results show that combining a highly active AMP and low-mol.-weight HPG yields bioconjugates with excellent biocompatibility, MICs below 100 μg/mL, and proteolytic stability, which could potentially improve its utility for in vivo applications. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Category: amides-buliding-blocks
The Article related to antimicrobial peptide polymer conjugate proteolysis biocompatibility, hyperbranched polyglycerol, antimicrobial peptide−polymer conjugates, aurein peptides, biocompatibility, bioconjugation, proteolysis and other aspects.Category: amides-buliding-blocks
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics