Antimicrobial peptides and compositions, methods, articles and kits relating thereto
Inventors
van Hoek, Monique L. • BISHOP, Barney M.
Assignees
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Publication Number
US-12384821-B2
Publication Date
2025-08-12
Expiration Date
Abstract
Peptides are described herein, in particular peptides having antimicrobial properties, as are compositions, articles, and kits comprising such peptides, and methods for using the peptides.
Core Innovation
The invention relates to antimicrobial peptide sequences and variants, including peptides defined by specific amino-acid sequences and a formula-based motif, where the C-terminal region contains LLRRFG (SEQ ID NO:12). The peptide variants include one or more substitutions, insertions, additions, or deletions while maintaining at least 80% homology to specified reference sequences, and some variants exclude SEQ ID NO:1.
The invention further describes peptide compositions and articles, including kits, polynucleotides encoding the peptides, and optional sequence modifications such as N-terminal acetylation and C-terminal amidation. The peptide and variant definitions are positioned around targeting microbial growth, including biofilm reduction and inhibition, and around binding lipopolysaccharide (LPS).
In documented embodiments, designed cathelicidin-derived peptides, including VK-CATH4.1 and VK-CATH4.2 and DRGN peptides, are evaluated for activity against carbapenem-resistant K. pneumoniae, with reported effects including MIC changes and identification of inactive variants that lack the LLRRFG-containing region described in the claims. The document also reports assay readouts associated with membrane permeabilization/depolarization, hemolysis, and circular dichroism helicity, as well as a Galleria mellonella infection model for antimicrobial performance.
Claims Coverage
The partial claim set includes three independent peptide claims. Across these claims, the main inventive features are the defined peptide sequences or sequence-motif frameworks, variant allowances with at least 80% homology, specified exclusion relationships, and retention of a C-terminal LLRRFG (SEQ ID NO:12) element.
Defined peptide with C-terminal LLRRFG-containing variant homology
A peptide of a specified sequence (RRWRRFFQKAKRLLRRFG (SEQ ID NO:6) or RRWRRFFRKAKRLLRRFG (SEQ ID NO:7)), or a variant sequence thereof with substitutions, insertions, additions, or deletions, wherein the C-terminal region of the variant contains LLRRFG (SEQ ID NO:12) and the variant sequence has at least 80% homology with SEQ ID NO:6 or SEQ ID NO:7.
Sequence-motif peptide with defined variable positions and exclusion of SEQ ID NO:1
A peptide comprising a sequence Xaa1RWRRFFXaa8KAKRXaa13Xaa14Xaa15Xaa16Xaa17Xaa18 (SEQ ID NO:5) with independently defined choices for multiple positions, or a variant sequence thereof comprising one or more substitutions, insertions, additions, or deletions, wherein the variant sequence is at least 80% homologous to SEQ ID NO:5 and wherein SEQ ID NO:5 or the variant sequence excludes SEQ ID NO:1.
Backbone peptide sequence variant restricted at Xaa18 with C-terminal LLRRFG and exclusion of SEQ ID NO:1
A peptide comprising FRWRRFFRKAKRFLKRHXaa18VSIAIGTVRLLRRFG (SEQ ID NO:3) where Xaa18 is an amino acid except glycine (G), or FRWRRFFRKAKRFLKRHAVSIAIGTVRLLRRFG (SEQ ID NO:4), or a variant sequence thereof comprising substitutions, insertions, additions, or deletions, wherein the variant sequence is at least 80% homologous to SEQ ID NO:3 or SEQ ID NO:4 and containing LLRRFG (SEQ ID NO:12) at the C-terminal region and excludes SEQ ID NO:1.
Across the independent claims, the coverage centers on specified peptide sequences and peptide frameworks defined by variable residue positions, each allowing substitutions, insertions, additions, or deletions while requiring at least 80% homology to defined reference sequences and requiring the C-terminal LLRRFG (SEQ ID NO:12) element, with certain claims also requiring exclusion of SEQ ID NO:1.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treatment and/or prevention of infections, including reducing microbial growth and biofilms.
Wound healing.
Endotoxemia treatment via binding lipopolysaccharide (LPS).
LPS detection/diagnosis using an LPS binding complex.
Use of antimicrobial peptides, including designed cathelicidin-derived peptides, evaluated against carbapenem-resistant K. pneumoniae.
Assessment of antimicrobial performance using a Galleria mellonella infection model.
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