121st General Meeting of the KCS

Type Poster Presentation
Area Inorganic Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code INOR.P-205
Subject Ultrastable cross-bridged chelators as general platform for antibody radiolabeling with Cu-64
Authors Swarbhanu Sarkar, Rammyani Pal1, Yeong Su Ha1, Phoung Tu Huynh1, Woonghee Lee1, Jung-Min Jung1, JUNG-YOUNG KIM2, Kyo-Chul Lee2, Jeongsoo Yoo1,*
Molecular Medicine, School of Medicine, Kyungpook National University, Korea
1Molecular Medicine, BK21 Plus KNU Biomedical Convergence Program, School of Medicine, Kyungpook National University, Korea
2RI-Convergence Research, Korea Institute of Radiological & Medical Science, Korea
Abstract Monoclonal antibodies have been widely exploited for both diagnostic and therapeutic purposes. For antibody radiolabeling with Cu-64, requirement of a bifunctional chelator which can hold the radio metal robustly is essential. Thus development of ultrastable chelator is needed. However, most heat-sensitive antibodies cannot be radiolabeled utilizing these chelators because of their high temperature radiolabeling profile. It thus limits its wide applications. Herein we develop a new type of versatile cross-bridged macrocyclic chelator (PCB-TE2A-alkyne), which can be transformed to any functional group prior to radiolabeling for easy conjugation with antibody. Modifications to different functionality did not require any tedious purification and after radiolabeling it can be conjugated to antibody in excellent yield. It thus facilitates a general and broad platform for antibody radiolabeling with Cu-64. The applicability was demonstrated using trastuzumab in NIH3T6.7 tumor-bearing BALB/c nude mice.
E-mail swarbhnau.sarkar@gmail.com