Targeted G-quadruplex polypeptide PET imaging agent as well as preparation method and application thereof

• Main Authors: HUANG SHUN, SHI DAZHI, TANG GANGHUA, WU HUBING, HAN YANJIANG
• Format: Patent
• Language: Chinese; English
• Published: 29.07.2022
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

The invention discloses a targeted G-quadruplex polypeptide PET imaging agent and a preparation method and application thereof.The PET imaging agent is an excellent novel pharmacokinetic probe and structurally comprises polypeptide, metal chelating groups and radioactive metal nuclides, the preparation method is simple, convenient and rapid, the yield is high, and the PET imaging agent is good in stability, high in water solubility and high in in-vivo blood removal speed and has good application prospects. The PET imaging agent can be specifically taken in tumor parts mainly through kidney and liver metabolism, and can be widely applied to biological function imaging. 本发明公开了一种靶向G-四链体多肽类PET显像剂及其制备方法与应用，该PET显像剂是优良的药代动力学新型探针，其结构包括多肽、金属螯合基团和放射性金属核素，其制备方法简便快捷，产率较高，该PET显像剂稳定性好、水溶性强，体内血液清除快，主要经肾脏、肝脏代谢，能特异性摄取于肿瘤部位，该PET显像剂可广泛应用于生物学功能显像中。