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  • 09월 05일 17시 이후 : 초록수정 불가능, 일정확인 및 검색만 가능

제120회 대한화학회 학술발표회, 총회 및 기기전시회 안내 Synthesis of novel multi-chelator tether for mAb radiolabeling

2017년 9월 5일 15시 44분 31초
MEDI.P-369 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
10월 19일 (목요일) 11:00~12:30
Medicinal Chemistry
저자 및
Hyeonsu Na, Heejung Kim1, ILJUNG LEE1,*, Eunbi Shin1, Dong Wook Kim*, Jai Woong Seo2
Department of Chemistry, Inha University, Korea
1Korea Institute of Radiological & Medical Science, Korea
2Department of Biomedical Engineering, University of California, Davis, United States
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승인 1건
Bioorthogonal chemistry has been exploited in tagging diverse biomolecules such as intra/intercellular or membrane proteins. Non-invasive in vivo immune-PET (Positron Emission Tomography) has also been benefited by advanced labeling methods derived from bioorthogonal chemistry. The specific activity of monoclonal antibody (mAb) relies on the number of radiometal chelator conjugated on mAb. Although several number of amine or cysteine on mAb can be functionalized with NHS- or maleimide-chelator, there are limited number of available amines for radiolabeling. High chelator/mAb ratio often impedes an intact binding avidity by blocking the functional amine on mAb. Here we designed and synthesized mAb conjugated with multiple chelators, called multi-chelator tether, via inverse electron demand Diels-Alder(IEDDA) reaction. Multi-chelator tether may increase the specific activity of radiolabeled mAb without depleting available amines on the mAb and provide a high target signal to background ratio in tumor mouse model.