Topological modification of interleukin-2 and application of interleukin-2 as autoimmune disease medicine

• Main Authors: HE JING, XIAO XIAN, TIAN XIBAO, ZHANG WENBIN, LI ZHANGUO, FENG RUILING, FANG JING
• Format: Patent
• Language: Chinese; English
• Published: 07.11.2023
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention discloses topological transformation of interleukin-2 and application of the interleukin-2 as an autoimmune disease medicine. According to the invention, the interleukin-2 is subjected to topological transformation, so that the interleukin-2 with a cyclic or isohydrocarbon topological structure of targeted activated Treg is obtained. The affinity of the interleukin-2 with the cyclic or Soxhlet-hydrocarbon structure and a receptor is not changed, the half-life period of the medicine can be prolonged, the stability can be enhanced, the dosage of long-term medication and the medication frequency can be reduced, and the effect of inhibiting immunity can be achieved. As a long-acting immunosuppressor, the interleukin-2 topological transformation protein disclosed by the invention is beneficial to treatment of various autoimmune diseases. 本发明公开了白细胞介素-2的拓扑改造及其作为自身免疫病药物的应用。本发明对白细胞介素-2进行拓扑改造，获得了靶向性激活Treg的环状或索烃拓扑结构的白细胞介素-2。环状或索烃结构的白细胞介素-2不改变其与受体的亲和性，同时可以延长药物的半衰期，增强稳定性，减少长期用药的剂量和用药次数，发挥抑制免疫的效果。本发明的白细胞介素-2拓