Defensin fragments for use in therapy or prophylaxis
AssigneeAesculus Bio ApS
InventorsJan Wehkamp, Dirk Ehmann
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Abstract
The present invention relates to new peptides derived from HD-5 or HNP-4 having antimicrobial activity for use in modulating the microbiome of intestines, the lungs, the skin, the mouth, the eye, the ear, the vagina or other bodily surfaces and/or for use as an antimicrobial agent in a human or other mammals, as well as to medicaments containing these peptides.
Claims22
Peptide having antimicrobial activity, which peptide is a fragment of HD-5, wherein the peptide consists of the sequence of:
- (SEQ ID No. 1)
- ATCYCRTGR,
- (SEQ ID No. 2)
- RGTRCYCTA,
- (SEQ ID No. 5)
- Ac-atcycrtGr-NH2,
- (SEQ ID No. 41)
- LYRLCCR,
- (SEQ ID No. 34)
- ATCYCRTGRCATR,
- (SEQ ID No. 12)
- ATCYCRTGRCATRESLSGVCEISGRLYR,
- (SEQ ID No. 14)
- TGRCATRESLSGVCEISGRLYRLCCR,
- (SEQ ID No. 19)
- CATRESLSGVCEISGRLYRLCCR,
- (SEQ ID No. 25)
- ESLSGVCEISGRLYRLCCR,
- or
- (SEQ ID No. 28)
- CATRESLSGVCEISGRLY.
The peptide of any of the preceding claims, wherein the peptide is a homodimer linked through a cystin-bridge, preferably wherein said homodimer is a dimer of HD-51-9.(SEQ ID No. 1).
The peptide of any of the preceding claims, comprising an N-terminal modification, preferably selected from acetyl-, formyl-, pyroglutamyl-, fatty acids-, urea-, carbamate-, and alkylamine.
The peptide of any of the preceding claims, comprising a the C-terminal modification, preferably selected from one of the group consisting of:
- -Amide, -Acid, -N-alkyl-Amide, -Aldehyde, -Ester, -p-Nitroanilide, and -7-Amino-4-Methylcoumarin.
The peptide as claimed in any of the preceding claims, wherein the peptide consists of or comprises D-and/or L-amino acids.
Peptide having antimicrobial activity, which peptide is a fragment of HNP-4, consisting of the sequence of:
- VCSCRLVFCRR (SEQ ID No. 3), SEQ ID No. 3, RRCFVLRCSCV (SEQ ID No. 4), or Ac-vcscrlvfcrr-NH2 (SEQ ID NO. 6).
The peptide as claimed in any of the preceding claims, wherein the peptide comprises N- and/or C-terminal modifications, preferably wherein said modification is an N-terminal acetyl modification and/or a C-terminal amide modification.
A method of manufacturing the peptides of any of the preceding claims, the method comprising subjecting reduced HD5 or HNP-4 to protease activity followed by purification.
Dependencies are inferred from the claim text.