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Exact(6)
Cyclic peptides were active only toward X. vesicatoria and P. syringae, being c KLKLKFKLKQ) (BPC10L) the most active peptide with MIC values of 6.25 and 12.5 μM, respectively.
The most active peptide, H-Asp-cyclo[Orn-Phe-Trp-Lys-Tyr-Asp]-Val-OH (3), is approximately 2 logs less potent than hU-II (pD2=6.3 vs 8.4).
The most active peptide was further evaluated in vitro for RANKL induced osteoclastogenesis in mouse macrophage cells, and in vivo for Freund's complete adjuvant induced arthritis (AIA) in Lewis rats.
First, N-acylation of the most active peptide III using 4 different acyl groups (See Fig. 2b) was performed.
BP100.2mi was the most active peptide and BP100.2 and BP100.3 were the least active BP100 derivatives in this assay.
LTX-315 was the most active peptide against the lymphoma cells with IC50 values ranging from 10 to 23 μM compared to LTX-302 (IC50 values ranging from 31 to 46 μM) and LTX-318 (IC50 values ranging from 73 to 106 μM) (Table 3).
Similar(54)
A series of CHR-derived peptides were stabilized by the introduction of one (e.g. HIV C14 Linkmid)[ 216] or two lactam cross-links (e.g. HIV31, Figure 19 b).[ 434] In cell-based assays, the most active peptides in these series exhibit micromolar inhibitory activities against viral infection.
Cytotoxicity, bactericidal activity and stability towards protease degradation of the most active peptides were also determined.
When the two most active peptides, PIP-18[59 76] PIP-18[59 76]IP[59–67], were andlied topically at a 150 mg/kg dose for testing wound healing activity in a mouse model of S. aureus infection, the former accelerates faster wound healing than the latter peptide at 14 days post-treatment.
As an example, a plot of the concentration-dependent growth inhibition of one of the most active peptides, peptide 5, is shown in Figure 2a, with the MIC of 8 μg/mL indicated by the arrow.
Our most active antiviral peptide, GRFN-1, contained a largely intact loop region (–24RSGSYLDN31–) modified only by the chemically conservative substitution of Leu by cyclohexylalanine.
Related(20)
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