Peking Union Medical College Hospital; Chinese Academy Of Medical Sciences
发明人:
申请号：
EP18787253.6
公开号：
EP3613441A1
申请日:
2018.04.12
申请国别(地区):
EP
年份:
2020
代理人:
摘要：
The present invention discloses a targeting polypeptide compound having dual targets, comprising a TATE cyclic peptide structure, an RGD cyclic peptide structure and a NOTA chelating group, wherein the TATE cyclic peptide structure, the RGD cyclic peptide structure and the NOTA chelating group are respectively linked by a PEG segment having a polymerization degree of 1 to 5 or directly linked to a same glutamic acid molecule； the structure of the polypeptide compound can be simplified represented as NOTA-PEGn-Glu{PEGm-TATE}-PEGP-RGD, where m, n and p are an integer from 0 to 5 respectively. The prresent invention further discloses a TATE-RGD dual-target radioactive molecular probe based on the polypeptide compound. The TATE-RGD dual-target polypeptide drug of the present invention may simultaneously bind to SSTR, integrin αvβ3, has higher receptor binding affinity and uptake, more excellent non-target tissue clearance rate, and better in vivo and in vitro stability. The invention further discloses a method for preparing the compound and radioactive probe and applications thereof.
