Abstract: The invention relates to the use of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto at least two bulky and lipophilic groups and having at least one more cationic than anionic moiety, in the manufacture of a medicament for destabilizing microbial cell membranes and the use as a membrane acting antimicrobial agent of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto a super bulky and lipophilic group comprising at least 9 non-hydrogen atoms and having at least two more cationic than anionic moieties and to methods of treatment involving such molecules, in particular peptides including peptide derivatives, and peptidomimetics.

Abstract: The present invention relates to a peptide or peptidomimetic for use in the treatment of a biofilm-associated infection in a subject, wherein said peptide or peptidomimetic a) carries a net positive charge, b) is 1 to 6 amino acids in length or is an equivalently sized peptidomimetic; and c) is amphipathic in nature, having one or more lipophilic groups, one of said lipophilic groups comprising at least 7 non-hydrogen atoms.

Abstract: The present invention relates to a compound of formula (I) AA-AA-AA-X—Y—Z wherein, in any order, 2 of said AA (amino acid) moieties are cationic amino acids and 1 of said AA is an amino acid with a lipophilic R group, the R group having 14-27 non-hydrogen atoms; X is a N atom, which may be substituted by a branched or unbranched C1-C10 alkyl or aryl group which group may incorporate up to 2 heteroatoms selected from N, O and S; Y represents a group selected from —Ra—Rb—, —Ra—Rb—Rb— and —Rb—Rb—Ra— wherein Ra is C, O, S or N, and Rb is C; each of Ra and Rb may be substituted by C1-C4 alkyl groups or unsubstituted; and Z is a group comprising 1 to 3 cyclic groups each of 5 or 6 non-hydrogen atoms, 2 or more of the cyclic groups may be fused and one or more of the cyclic groups may be substituted; the Z moiety incorporates a maximum of 15 non-hydrogen atoms; and wherein the bond between Y and Z is a covalent bond between Ra or Rb of Y and a non-hydrogen atom of one of the cyclic groups of Z.

Abstract: The present invention relates to a method of improving the resistance of a peptide or peptidomimetic to degradation by trypsin which comprises incorporating into said peptide or peptidomimetic a C-terminal capping group of formula (I): X—Y—Z (I) wherein X is a N atom, which may be substituted by a branched or unbranched C1-C10 alkyl or aryl group which group may incorporate up to 2 heteroatoms selected from N, O and S; Y represents a group selected from —Ra—Rb—, —Ra—Rb—Rb,- and —Rb—Rb—Ra— wherein Ra is C, O, S or N, and Rb is C; each of Ra and Rb, may be substituted by C1-C4 alkyl groups or unsubstituted; and Z is a group comprising 1 to 3 cyclic groups each of 5 or 6 non-hydrogen atoms, 2 or more of the cyclic groups may be fused and one or more of the cyclic groups may be substituted; the Z. moiety incorporates a maximum of 15 non-hydrogen atoms; and wherein the bond between Y and Z is a covalent bond between Ra or Rb of Y and a non-hydrogen atom of one of the cyclic groups of Z.

Abstract: The invention relates to the use of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto at least two bulky and lipophilic groups and having at least one more cationic than anionic moiety, in the manufacture of a medicament for destabilising microbial cell membranes and the use as a membrane acting antimicrobial agent of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto a super bulky and lipophilic group comprising at least 9 non-hydrogen atoms and having at least two more cationic than anionic moieties and to methods of treatment involving such molecules, in particular peptides including peptide derivatives, and peptidomimetics.

Abstract: The present invention provides a cytotoxic 7 to 25-mer peptide with three or more cationic residues which has one or more non-generic bulky and lipophilic amino acids, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing the peptides, pharmaceutical compositions containing them, and their use as medicaments, particularly as antibacterial or antitumor agents.

Abstract: The present invention provides a cytotoxic 7 to 25-mer peptide with three or more catonic residues which has one or more non-genetic bulky and lipophilic amino acids, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing the peptides, pharmaceutical compositions containing them, and their use as medicaments, particularly as antibacterial or antitumor agents.

Abstract: The present invention relates to a method of producing a bioactive peptide, wherein the peptide is 7 to 25 amino acids in length, has at least 3 cationic amino acids and is capable of forming an amphipathic ?-helix, which method comprises identification of a cationic sector and division of the remaining part of the peptide into three further sectors which are substantially equal in size, and incorporation of at least 60% of the bulk and lipophilicity provided by the amino acid R groups into the sectors flanking the cationic sector; and to uses of the peptides produced thereby in therapy, particularly in the treatment of benign or malignant tumours.

Abstract: The invention relates to the use of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto at least two bulky and lipophilic groups and having at least one more cationic than anionic moiety, in the manufacture of a medicament for destabilizing microbial cell membranes and the use as a membrane acting antimicrobial agent of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto a super bulky and lipophilic group comprising at least 9 non-hydrogen atoms and having at least two more cationic than anionic moieties and to methods of treatment involving such molecules, in particular peptides including peptide derivatives, and peptidomimetics.

Abstract: The present invention provides a modified lactoferrin peptide which is cytotoxic, 7 to 25 amino acids in length, with three or more cationic residues and which has one or more extra bulky and lipophilic amino acids as compared to the native lactoferrin sequence, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing such peptides, pharmaceutical compositions containing such peptides and use of the peptides as medicaments, particularly as antibacterials or anti-tumoural agents.

Abstract: The invention relates to the use of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto at least two bulky and lipoophilic groups and having at least one more cationic than anionic moiety, in the manufacture of a medicament for destabilising microbial cell membranes and the use as a membrane acting antimicrobial agent of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto a super bulky and lipophilic group comprising at least 9 non-hydrogen atoms and having at least two more cationic than anionic moieties and to methods of treatment involving such molecules, in particular peptides including peptide derivatives, and peptidomimetics.

Abstract: The present invention provides a cytotoxic 7 to 25-mer peptide with three or more catonic residues which has one or more non-genetic bulky and lipophilic amino acids, as well as esters, amides, salts and cyclic derivatives thereof as well as methods of preparing the peptides, pharmaceutical compositions containing them, and their use as medicaments, particularly as antibacterial or antitumor agents.