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Understanding the mechanism of action of antimicrobial peptides is pivotal to the design of new and more active peptides.
Conjugation of the cell penetrating hepta-arginine vector to their N- or C-termini through two glycine residues resulted in more active peptides, which also permeabilized the red blood cells with a relatively high plasma membrane potential generated in the presence of valinomycin.
However the two cyclization strategies employed have different effects, with disulfide cyclization resulting in more active peptides while backbone cyclization results in more proteolytically stable peptides.
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Their activity, however, was not significantly higher than that of the unmodified tripeptides and the combined use with the more active peptide-MLE Ac-FR-NH2 did not show any cooperativity (data not shown).
On a molar basis, ET-1[1-32] appears to be a more active peptide than the 21-amino acid ET-1 (7).
The graph increases more rapidly as active peptides have larger Tanimoto coefficient than non-active peptides.
The best scoring complexes were also used to identify key residues of both interacting partners, indicating that such an approach should help the design of more active and/or selective peptide blockers of targeted ion channels.
It is known that CII peptide fragments derived from the cyanogen bromide digestion of native CII are immunologically more active than chemically synthesized peptides [ 24, 25].
We are confident that ongoing work to identify peptides more active against P. falciparum will allow mosquitoes with significantly reduced transmission of human malaria to be generated in the near future.
As a trend, ester derivatives are slightly more active than amides while heterochiral peptides are more active than their homochiral diastereoisomer.
Fusion of the template peptide and the stabilized peptide to the cell-penetrating peptide TAT produced more active but equally potent inhibitors of cap-dependent translation in cell lines.
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CEO of Professional Science Editing for Scientists @ prosciediting.com