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Methods for synthesizing conformationally constrained peptides, peptidometics and the use thereof as synthetic vaccines

机译:构象受限的肽,拟肽的合成方法及其作为合成疫苗的用途

摘要

The present invention relates to methods for synthesizing conformationally constrained peptides and cyclic peptidomimetics obtainable by these methods which are conformationally constrained due an internal cross-link. This cross-link is formed between the side chain of an amino acid residue or analog and a (2S,4S)-4-functionalized proline residue. The invention further relates to the use of (2S,4S)-4-functionalized proline residues as building units in the synthesis of such peptidomimetics and to the use thereof as antigens, alone or in combination with suitable immunopotentiating delivery systems, for example immunopotentiating reconstituted influenza virosomes to elicit an immune response in a mammal. Moreover, the invention also relates to pharmaceutical compositions containing the same. IMAGE
机译:本发明涉及合成构象受限的肽的方法和可通过这些方法获得的环状肽模拟物,所述环状拟肽由于内部交联而被构象受限。该交联在氨基酸残基或类似物的侧链与(2S,4S)-4-官能化的脯氨酸残基之间形成。本发明进一步涉及(2S,4S)-4-官能化的脯氨酸残基在此类肽模拟物的合成中的用途,以及其作为抗原的用途,其单独或与合适的免疫增强递送系统(例如重组的免疫增强性)组合使用流感病毒体在哺乳动物中引发免疫反应。此外,本发明还涉及包含该药物组合物的药物组合物。 <图像>

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