Maleimide group-modified angiogenesis inhibitor HM-1 and application thereof

The invention discloses a maleimide group-modified angiogenesis inhibitor HM-1 and application thereof, which belong to the technical field of polypeptide drugs. The invention chooses an appropriate maleimide group to modify the N terminal of angiogenesis inhibitor polypeptide HM-1, the sequence tar...

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Bibliographische Detailangaben
Hauptverfasser: KANG ZHI'AN, WANG KEQUAN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a maleimide group-modified angiogenesis inhibitor HM-1 and application thereof, which belong to the technical field of polypeptide drugs. The invention chooses an appropriate maleimide group to modify the N terminal of angiogenesis inhibitor polypeptide HM-1, the sequence targets of the obtained polypeptides X1-X90 are not changed, moreover, the in-vivo half-life of polypeptide molecules is prolonged, the clearance rate is low, and immunogenicity and antigenicity are decreased. The maleimide group-modified angiogenesis inhibitor HM-1 can be used for preventing and treating tumors, various inflammations and neovascular eye diseases. Moreover, anti-tumor activity is kept unchanged, but the plasma concentration at the diseased region is increased, so that the frequencyof administration is decreased. The maleimide group-modified HM-1 is administrated once every seven days rather than twice every day in the past. 本发明公开了种马来酰亚胺基团修饰的血管生成抑制剂HM-1及其应用,属于多肽药物技术领域。本发明选择合适的马来酰亚胺基团对血管生成抑制剂多肽HM-1的N端进行