C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 7/64 (2006.01) A61K 38/08 (2006.01) A61K 38/12 (2006.01) A61P 31/04 (2006.01) A61P 31/12 (2006.01) C07K 7/06 (2006.01)
Patent
CA 2589833
The present invention provides cyclic and linear short peptides containing one of the following amino acid sequences: K(2~Nal)RR(2-Nal)I (SEQ ID NO: 1), K(2- Nal)RR(2-Nal)V (SEQ ID NO:2), K(2-Nal)IK(2-Nal)R (SEQ ID NO:3), K(2- Nal)RR(2~Nal)VR(2-Nal)I (SEQ ID NO:4), I(2-Nal)RV(2-Nal)RR(2-Nal)K (SEQ ID NO:5), K(1-Nal)RR(1-Nal)VR(1-Nal)I (SEQ ID NO:6), and K(Bip)RR(Bip)VR(Bip)I (SEQ ID NO: 7), wherein 1-Nal represents (naphtha-1-yl)alanine, 2-Nal represents (naphtha-2-yl)alanine and Bip represents (4,4'-biphen-yl)alanine. The peptides exhibit broad spectrum antimicrobial activity against Gram- positive and Gram-negative bacteria and fungi, with improved serum compatibility and reduced hemolysis.
La présente invention décrit des peptides courts linéaires et cycliques qui contiennent l~une des séquences d~acides aminés suivantes : K(2Nal)RR(2-Nal)I (SEQ ID NO: 1), K(2-Nal)RR(2-Nal)V (SEQ ID NO:2), K(2-Nal)IK(2-Nal)R (SEQ ID NO:3), K(2-Nal)RR(2Nal)VR(2-Nal)I (SEQ ID NO:4), I(2-Nal)RV(2-Nal)RR(2-Nal)K (SEQ ID NO:5), K(1-Nal)RR(1-Nal)VR(1-Nal)I (SEQ ID NO:6), et K(Bip)RR(Bip)VR(Bip)I (SEQ ID NO: 7), où 1-Nal représente la (naphta-1-yl)alanine, 2-Nal représente la (naphta-2-yl)alanine et Bip représente la (4,4~-biphényl)alanine. Lesdits peptides présentent une activité anti-microbienne à large spectre contre les bactéries Gram positives et Gram négatives, ainsi que les champignons. Ils présentent également une meilleure compatibilité avec le sérum et induisent moins d~hémolyse.
Cheng Jya-Wei
Tzeng Shiou-Ru
Oyen Wiggs Green & Mutala Llp
Pacgen Biopharmaceuticals Corporation
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