Peptoids, antimicrobial

Nc, S., Goodson, B., Ehrhardt, A., Moos, W. H., Siani, M., and Winter, J. Combinatorial discovery process yields antimicrobial peptoids. Bioorg. Med. 

Resistance to peptidases was also reported for the octapeptoid 6.106 when incubated with papain, chymotrypsin, or thermolysin [229], However, resistance to peptidases may not be synonymous with a long half-life in vivo, since many factors beside peptidases can be expected to contribute to the elimination of peptoids. An indirect indication of this effect can be found for antimicrobial peptoids and particularly compound CHIR29498 (6.107) [232], In mice infected with Staphyllococus aureus, this peptoid was less active when injected 2 h post-infection compared to 0 h or 0.5 h. The conclusion drawn by the authors was that the compound requires optimization for improved absorption or stability within the body. 

Statz Andrea R, Park Jong P, Chongsiriwatana Nathaniel P et al. (2008) Surface-immobilised antimicrobial peptoids. Biofouling 24 439 148... 

Ng et al. (154) reported the identification of several antimicrobial peptoids from an 845-member SP pool library organized as 65 pools of 13 compounds inspired by previous, larger combinatorial efforts (155). A 400-member SP library based on a 1,3-disubstimted cyclohexanone scaffold, prepared as 20 pools of 20 compounds, was reported by Abato et al. (156) a selective inhibitor of a serine protease, plasmin, was identified from iterative deconvolution of the library. 

Future Directions From Antimicrobial to Anticancer Peptoids 281... 

Bearing in mind that the thickness of the lipid bilayer of a bacterial membrane is approximately 30 A and that the antimicrobial activity and sdectivity of AMPs seemed to be driven predominantly by physiochemical parameters, in 2003 Patch and Barron designed peptoids to mimic the fadally amphipathic stmcture of the cationic, 23-mer AMP magainin-2. Magainin-2 has three distinct faces that are, respertivdy, rich in hydrophobic aliphatic residues, aromatic residues, and basic residues (lysines) (Figure 14). The threefold periodicity of... 

In 2008, Chongsiriwatana et al published a follow-up study on the previously reported antimicrobial peptoids. A second-generation peptoid library was designed, again, to mimic the amphipathic stmcture of magainin-2, this time... 

The CV assay is a good measure to screen the efficacy of antimicrobials against biofilms, except it does not provide information regarding the bacterial cell viability. To ensure that the peptoids were killing bacteria rather than just physically removing them from the stuface, the deaease in the cell viability was measured by bacterial plating for prevention of biofilm formation and reduction of existing biofilms. At 12.5 pM, peptoids 1 and showed similar effects to... 

One of the long-standing goals of foldamer research has been to mimic the function of biopolymers. While the focus has been on establishing the principles of folding, there have been some successes in designing shape-dependent function. For example, it was recently shown that p-peptides, peptoids, and simple polymers could capture the antimicrobial activity and selectivity of the natural host defense peptides [23-27]. As foldamer researchers develop more sophisticated stmctures, we expect many more examples. 

In recent years, peptoid research has focused on the development of new peptoid-based antimicrobial agents either from de novo design [20-24], cyclic peptoids [25], libraries [26,27], or by transforming naturally occurring antimicrobial peptides into peptoid analogs [28]. 

Godballe T, Nilsson LL, Petersen PD et al (2011) Antimicrobial a-peptides and a-peptoids. Chem Biol Drug Des 77 107-116... 

Ryge TS, Frimodt-MoUer N, Hansen PR (2008) Antimicrobial activities of twenty lysine-peptoid hybrids against clinically relevant bacteria and fungi. Chemotherapy 54 152-156... 

Goodson B, Ehrhardt A, Ng S, Nuss J et al (1999) Characterization of novel antimicrobial peptoids. Antimicrob Agents Chemother 43 1429-1434... 

Kapoor R, Eimerman PR, Hardy JW et al (2011) Efficacy of antimicrobial peptoids... 

Antimicrobial peptoids Are effective against peuAomonas aeruginosa biofilms. Antimicrob Agents Chemother 55 3054-3057... 

A comparison of linear and cyclic peptoid oligomers as potent antimicrobial agents. ChemMedChem 7 114-122... 

Humet M, Carbonell T, Masip I et al (2003) A positional scanning combinatorial library of peptoids as a source of biological active molecules identification of antimicrobials. J Comb Chem 5 597-605... 

Chongsiriwatana NP, Patch JA, Czyzewski AM et al (2008) Peptoids that mimic the structure, function, and mechanism of helical antimicrobial peptides. Proc Natl Acad Sci USA 105 2794-2799... 

Zhu WL, Hahm KS, Shin SY (2007) Cathelicidin-derived Trp/Pro-rich antimicrobial peptides with lysine peptoid residue (nlys) therapeutic index and plausible mode of action. J Pept Sci 13 529-535... 

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