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    • 1. 发明申请
    • NOVEL ANTIMICROBIAL PEPTIDES AND THEIR APPLICATION
    • 新型抗微生物肽及其应用
    • WO2009109156A3
    • 2010-04-29
    • PCT/CZ2009000034
    • 2009-03-03
    • USTAV ORGANICKE CHEMIE A BIOCHCEROVSKY VACLAVSLANINOVA JIRINAHOVORKA OLDRICHCVACKA JOSEFVOBURKA ZDENEKFUCIK VLADIMIRBEDNAROVA LUCIEVOTRUBA IVANBOROVICKOVA LENKATURANEK JAROSLAV
    • CEROVSKY VACLAVSLANINOVA JIRINAHOVORKA OLDRICHCVACKA JOSEFVOBURKA ZDENEKFUCIK VLADIMIRBEDNAROVA LUCIEVOTRUBA IVANBOROVICKOVA LENKATURANEK JAROSLAV
    • C07K7/08A61K38/10
    • C07K14/43572A61K38/00C07K7/08
    • This invention involves four novel peptides of the formulas I, II, III a IV isolated from natural sources and their synthetic analogs of general formula V and VI, where R 1 represents acyl, alkyl or unprotected amino group, R 2 represents amid, substituted amid, unprotected carboxylic group or ester, Xaa represents, independently from each other, proteinogenic amino acid, D-amino acid, non-standard amino acid or amino acid with the side chain modification, n means position of the amino acid replacement and m means the number of the replacements in the peptide chain, and their applications as antimicrobial, antiviral, antifungal, antiparasitic and anticancer compounds. Therefore, they are practical for the production of medication for the treatment of microbial, parasitic and fungal diseases and for the cancer treatment. Formulas for summary: H-Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-NH2 (I) H-VaI-Asn-Trp-Lys-Lys-VaI-Leu-GIy-Lys-IIe-IIe-Lys-VaI-AIa-Lys-NH2 (II) H-VaI-Asn-Trp-Lys-Lys-IIe-Leu-GIy-Lys-IIe-IIe-Lys-VaI-AIa-Lys-NH2 (III) H-Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val-Lys-NH2 (IV) R1-[Xaan]m -Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-R2 (V) R1-[Xaan]m-Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val-Lys-R2 (VI)
    • 本发明涉及从天然来源分离的四种分子式I,II,III和IV的新型肽及其通式V和VI的合成类似物,其中R 1表示酰基,烷基或未被保护的氨基,R 2表示氨基,取代的氨基 ,未被保护的羧基或酯,Xaa彼此独立地表示蛋白质氨基酸,D-氨基酸,非标准氨基酸或具有侧链修饰的氨基酸,n表示氨基酸置换的位置,m表示 肽链中的替代物的数量,以及它们作为抗微生物剂,抗病毒剂,抗真菌剂,抗寄生虫和抗癌化合物的应用。 因此,它们可用于生产用于治疗微生物,寄生虫和真菌疾病和癌症治疗的药物。 总结公式:H-Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-NH2(I) Asn-Trp-Lys-Lys-Val-Leu-Gly-Lys-IIe-IIe-Lys-Val-Ala-Lys-NH2(II)H-Val-Asn-Trp-Lys-Lys-IIe-Leu- Lys-IIe-IIe-Lys-Val-Ala-Lys-NH 2(III)H-Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val- NH 2(IV)R 1 - [Xanan] m -Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-R2 )R1- [Xanan] m-Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val-Lys-R2(VI)