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Protease-sensitive site in apolipoprotein A1, therapeutic and diagnostic implications

机译:载脂蛋白A1中蛋白酶敏感位点的治疗和诊断意义

摘要

The invention relates to the identification of a naturally occurring internal proteolytic cleavage site in the ApoA1 protein, which leads to inactivation of the mature protein. Specific modification of this cleavage site leads to a stabilised ApoA1 protein, which is beneficial for the reverse cholesterol transport. The invention therefore encompasses pharmaceutical compositions comprising a recombinant stabilised variant ApoA1 protein or rHDL particles comprising such a protein, for use in the treatment of patients having reduced HDL or hampered reverse cholesterol transport.
机译:本发明涉及ApoA1蛋白中天然存在的内部蛋白水解切割位点的鉴定,其导致成熟蛋白的失活。该切割位点的特异性修饰导致稳定的ApoA1蛋白,这对胆固醇的逆向转运是有益的。因此,本发明包括包含重组稳定的变体ApoA1蛋白或包含该蛋白的rHDL颗粒的药物组合物,用于治疗HDL降低或胆固醇逆向转运受阻的患者。

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