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HYDROPHOBIC MODIFIED preS-DERIVED PEPTIDES OF HEPATITIS B VIRUS (HBV) AND USE THEREOF AS HBV AND HDV ENTRY INHIBITORS
HYDROPHOBIC MODIFIED preS-DERIVED PEPTIDES OF HEPATITIS B VIRUS (HBV) AND USE THEREOF AS HBV AND HDV ENTRY INHIBITORS
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机译:疏水修饰的乙型肝炎病毒前导肽,并将其用作乙肝病毒和乙肝病毒进入抑制剂
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摘要
FIELD: chemistry.;SUBSTANCE: invention relates to biotechnology, specifically obtaining preS-derived peptides of hepatitis B virus (HBV) and can be used in medicine. The hydrophobic modified preS-derived peptide of hepatitis B virus (HBV) of formula: Hm-P-Kn, is used in preventing or treating HBV and/or HDV infections, primary infections of HBV and/or HDV, hepatitis B and/or D, chronic hepatitis B and/or D, where P is a preS-derived peptide, which is characterised by the amino acid sequence SEQ ID NO:11 or SEQ ID NO:12; H is a hydrophobic modification of peptide P, which is carried out at the N end of P and is selected from acylation and addition of hydrophobic functional components; R is a C-terminal modification of peptide P, which protects the peptide from degradation; m equals at least 1; n equals 0 or at least 1. The peptide can be bound with a label selected from a fluorescent dye, a radio isotope or a contrast substance, or is fused with a peptide or a protein, preferably selected from albumin and the Fc-domain of human IgG.;EFFECT: invention enables efficient inhibition of HBV and HDV entry into a cell.;15 cl, 12 dwg, 9 tbl, 1 ex
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机译:技术领域本发明涉及生物技术,特别是获得preS衍生的乙型肝炎病毒(HBV)肽,可用于医学领域。疏水性修饰的preS衍生的乙型肝炎病毒(HBV)肽,分子式为H m Sub> -PK n Sub>,用于预防或治疗HBV和/或HDV感染, HBV和/或HDV,乙型和/或丁型肝炎,慢性乙型和/或丁型肝炎的初次感染,其中P是preS衍生的肽,其特征在于氨基酸序列SEQ ID NO:11或SEQ ID NO :12; H是肽P的疏水修饰,其在P的N端进行,并且选自酰化和疏水功能组分的添加; R是肽P的C-末端修饰,其保护肽免于降解; m至少等于1; n等于0或至少1。肽可以与选自荧光染料,放射性同位素或造影剂的标记结合,或与肽或蛋白质(优选选自白蛋白和Fc的Fc结构域)融合人IgG;作用:本发明能够有效抑制HBV和HDV进入细胞。15cl,12 dwg,9 tbl,1 ex
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