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Protection of endogenous therapeutic peptides from peptidase activity through conjugation to blood components

机译:通过与血液成分结合,保护内源性治疗肽免受肽酶活性的影响

摘要

A secretin or secretin derivative protected against peptidase activity. The secretin or derivative comprises a peptidic sequence and a reactive group selected from the group consisting of succinimidyl and maleimido groups capable of reacting with an amino group, hydroxyl group or thiol group on a blood component to form a stable covalent bond. The reactive group is attached at a position along the peptidic sequence that provides, when conjugated to a blood component, a higher stability against peptidase degradation than the unconjugated secretin or derivative, and therefore an increased maintenance of the therapeutic activity compared to the unconjugated secretin or derivative. Such a compound is thus effective to provide a source of secretin having a high stability against peptidases. A method for synthesizing such a compound is also described.
机译:促胰液素或促胰液素衍生物防止肽酶活性。促胰液素或衍生物包含肽序列和选自由琥珀酰亚胺基和马来酰亚胺基组成的组的反应性基团,其能够与血液成分上的氨基,羟基或硫醇基反应以形成稳定的共价键。反应性基团沿着肽序列的位置连接,当与血液成分偶联时,与未偶联的促胰液素或衍生物相比,它对肽酶降解的稳定性更高,因此与未偶联的促胰液素或衍生物相比,治疗活性的维持性提高了衍生物。因此,这种化合物有效地提供了对肽酶具有高稳定性的促胰液素来源。还描述了合成这种化合物的方法。

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