Peptide inhibitors of toxins derived from LL-37

Details Peptide inhibitors of toxins derived from LL-37 Peptide inhibitors of toxins derived from LL-37

2004-01-27

2010-10-05

Carlson, Karen Cochrane (Department: 1656)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

C530S300000

Reexamination Certificate

active

07807617

ABSTRACT:
The invention relates to a peptidic compound with affinity to bacterial and fungal toxins, especially to lipopolysaccharide or lipoteichoic acid. The peptidic compound includes an amino acid sequence X1KEFX2RIVX3RIKX4FLRX5LVX6, wherein X1represents the N-terminal part: X2is K or E; X3is Q or E; X4is D or R; X5is N or E; X6represents the C-terminal part: an amino acid of the core sequence is optionally derivatized; the N-terminal part is acetylated, and/or the C-terminal part is amidated, and/or the sequence differs from the native amino acid sequence X1KEFKRIVQRIKDFLRNLVX6.

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Gennaro et al. 2000; Structural features and biological activities of the cathelicidin-derived antimicrobial peptides. Biopoly 55: 31-49.
Sawa et al. 1998; Evaluation of antimicrobial and lipolysaccharide-neutralizing effects of a synthetic CAP18 fragment againstPseudomonas aeruginosain a mouse model. Antimicrobial AGnents and Chemotherapy 42(12): 3269-3275.
Gutsmann, E.A., et al., “Interaction of CAP18-derived peptides with membranes made from endotoxins or phospholipids”,Biophysical Journal2001, 80:2935-2945.
Kirikae, T., et al., “Protective effects of a human 18-kilodalton cationic antimicrobial protein (CAP18)-derived peptide against murine endotoxemia”,Infection and Immunity, United States 1998, 66(5):1861-1868.
Nagaoka, Isao, et al., “Augmentation of the lipopolysaccharide-neutralizing activities of human cathelicidin CAP18/LL-37-derived antimicrobial peptides by replacement with hydrophobic and cationic amino acid residues”,Clinical and Diagnostic Laboratory Immunology2002, 9(5):972-982.

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