초록 ▼

The invention relates to the use of ubiquicidine or optionally modified peptide fragments derived therefrom for the preparation of a drug for the treatment, diagnostics or prophylaxis of infections in humans and animals. A peptide fragment derived from ubiquicidine comprises for instance a preferabl

The invention relates to the use of ubiquicidine or optionally modified peptide fragments derived therefrom for the preparation of a drug for the treatment, diagnostics or prophylaxis of infections in humans and animals. A peptide fragment derived from ubiquicidine comprises for instance a preferably continuous series of at least 3, preferably at least 7-13 amino acids from the amino acid sequence of ubiquicidine; KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVPTFGKKKGPN ANS (SEQ ID NO: 1). Hybrid molecules comprise for instance a cationic peptide with an antimicrobial action and/or a peptide fragment of ubiquicidine and/or a derivative thereof and one or more effector molecules.

대표청구항 ▼

1. Peptide fragment derived from ubiquicidine having antimicrobial activity and comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine:KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVPTFGKKKGPN ANS, (SEQ ID NO: 1) which does not include peptides havi

1. Peptide fragment derived from ubiquicidine having antimicrobial activity and comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine:KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVPTFGKKKGPN ANS, (SEQ ID NO: 1) which does not include peptides having the amino acid sequence KVHGSLARAGKVRGQTPKVAKQ (SEQ ID NO: 10) or AGKVRGQTPKVAKQEKKKKKT (SEQ ID NO: 11). 2. Peptide fragment as claimed in claim 1, comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine:KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVPTFGKKKGPN ANS, (SEQ ID NO: 1) which does not include peptides having the amino acid sequence KVHGSLARAGKVRGQTPKVAKQ (SEQ ID NO: 10) or AGKVRGQTPKVAKQEKKKKKT (SEQ ID NO: 11). 3. Peptide fragment as claimed in claim 1, consisting of the following amino acid sequences:ubiquicidine (1-18)KVHGSLARAGKVRGQTPK (SEQ ID NO: 2)ubiquicidine (29-41)TGRAKRRMQYNRR (SEQ ID NO: 3)ubiquicidine (18-29)KVAKQEKKKKKT (SEQ ID NO: 4)ubiquicidine (18-35)KVAKQEKKKKKTGRAKRR (SEQ ID NO: 5)ubiquicidine (29-35)TGRAKRR (SEQ ID NO: 7)ubiquicidine (42-59)FVNVVPTFGKKKGPNANS (SEQ ID NO: 8)ubiquicidine (36-41)MQYNRR (SEQ ID NO: 9).4. Derivative of ubiquicidine or of a peptide fragment derived from ubiquicidine having antimicrobial activity and comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine:KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVPTFGKKKGPNA NS, (SEQ ID NO: 1) which derivative has an amino acid sequence which is at least partly the reverse of the amino acid sequence of the corresponding original peptide. 5. Derivative of a ubiquicidine or of a peptide fragment derived from ubiquicidine having antimicrobial activity and comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine:KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVPTFGKKKGPNA NS, (SEQ ID NO: 1) wherein at least one of the amino acids from the original peptide is replaced by a stereoisomer of that amino acid. 6. Derivative of ubiquicidine or of a peptide fragment derived from ubiquicidine having antimicrobial activity and comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine:KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVPTFGKKKGPNA NS, (SEQ ID NO: 1) wherein the original amino acid chain is extended at one or both ends thereof with one or more groups, such as D-amino acids, protecting against degradation. 7. Derivative as claimed in claim 6, wherein the original amino acid chain is extended at one or both ends thereof with one or more groups of D-alanine.8. A method for the therapy of an infection in humans and animals, comprising:a) administering an antimicrobial compound having antimicrobial activity selected from the group consisting of ubiquicidine, a derivative of ubiquicidine, and a peptide fragment derived from ubiquicidine and comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine: KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVP TFGKKKGPNANS (SEQ ID NO: 1); and b) treating the infection, wherein the antimicrobial action of the compound results in inhibiting or otherwise exerting a negative effect on the infection. 9. The method of claim 8, wherein the peptide fragment comprises a peptide fragment, comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine:KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVPTFGKKKGPN ANS, (SEQ ID NO: 1) with the exception of peptides having the amino acid sequence KVHGSLARAGKVRGQTPKVAKQ (SEQ ID NO: 10) or AGKVRGQTPKVAKQEKKKKKT (SEQ ID NO: 11). 10. The method of claim 8, wherein the derivative comprises a derivative of ubiquicidine or of a peptide fragment derived from ubiquicidine and comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine:KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVPTFGKKKGPN ANS, (SEQ ID NO: 1) which derivative has an amino acid sequence which is at least partly the reverse of the amino acid sequence of the corresponding original peptide. 11. The method of claim 8, wherein the microbial infection is caused by a microorganism selected from the group consisting of Gram-positive bacteria, Gram-negative bacteria, fungi and viruses.12. Antimicrobial agent, comprising at least a suitable quantity of one or more active components chosen from ubiquicidine and/or peptide fragments derived from ubiquicidine, said ubiquicidine and/or said peptide fragments derived from ubiquicidine having antimicrobial activity, and comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine:KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVPTFGKKKGPN ANS (SEQ ID NO: 1). 13. The method of claim 8, wherein the compound comprises an antimicrobial agent, comprising at least a suitable quantity of one or more active components chosen from ubiquicidine, peptide fragments derived from ubiquicidine and comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine:KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVPTFGKKKGPN ANS (SEQ ID NO: 1). 14. Method for monitoring a treatment, comprising:a) administering an antimicrobial agent having antimicrobial activity, comprising at least a suitable quantity of one or more active components chosen from ubiquicidine, peptide fragments derived from ubiquicidine and comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine: KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVP TFGKKKGPNANS (SEQ ID NO: 1), b) observing the localization of the agent in time, and c) following the effect of the treatment, wherein the antimicrobial action of the compound results in inhibiting or otherwise exerting a negative effect on the infection. 15. Antimicrobial agent as claimed in claim 12, further comprising at least one excipient.16. Method for providing prophylactic action against an infection in humans or animals, comprising:a) administering a peptide fragment, derived from ubiquicidine having antimicrobial activity and comprising a continuous series of between 6 to 18 amino acids from the amino acid sequence of ubiquicidine: KVHGSLARAGKVRGQTPKVAKQEKKKKKTGRAKRRMQYNRRFVNVVP TFGKKKGPNANS, (SEQ ID NO: 1) which does not include peptides having the amino acid sequence KVHGSLARAGKVRGQTPKVAKQ (SEQ ID NO: 10) or AGKVRGQTPKVAKQEKKKKKT (SEQ ID NO: 11) in the form of a coating, wherein said administration results in preventing the infection.