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antagonists of interleukin-6 (il-6), which consist of soluble forms of the receptor alpha of il-6, changing the interface that binds to gp 130

机译:白细胞介素6(IL-6)的拮抗剂,由IL-6受体α的可溶性形式组成,改变与gp 130结合的界面

摘要

These are antagonists of interleukin-6, characterised in that they consist of soluble forms of the receptor alpha of human IL-6 (shIL-6R alpha ) containing one or more mutation in the gp130 binding interface. In a preferred embodiment, the mutations are present in a position chosen from the group comprising Ala 228, Asn 230, His 280 and Asp 281. These antagonists can be used as agents capable of preventing and treating diseases caused by abnormal IL-6 activity. The figure shows the antagonist activity of the mutant Ala228Asp/Asn 230Asp/His280Ser/Asp281Val in comparison with the agonist properties of wild type shIL-6R alpha . This antagonist can be used for preparation of drugs for the prevention, control and treatment of diseases caused by abnormal IL-6 bioactivity.
机译:它们是白介素6的拮抗剂,其特征在于它们由人IL-6的受体α的可溶形式(shIL-6Rα)组成,在gp130结合界面中包含一个或多个突变。在一个优选的实施方案中,所述突变存在于选自Ala 228,Asn 230,His 280和Asp 281的位置。这些拮抗剂可以用作能够预防和治疗由异常IL-6活性引起的疾病的试剂。该图显示了与野生型shIL-6Rα的激动剂性质相比,突变体Ala228Asp / Asn 230Asp / His280Ser / Asp281Val的拮抗活性。该拮抗剂可用于制备预防,控制和治疗由异常IL-6生物活性引起的疾病的药物。

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