A novel bifunctional maleimido CHX-A″ chelator for conjugation to thiol-containing biomolecules
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- 作者：Heng Xu ; Kwamena E. Baidoo ; Karen J. Wong ; Martin W. Brechbiel
- 关键词：Monoclonal antibody ; Thiol-maleimide chemistry ; Imaging and/or therapies of cancer
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2008
- 出版时间：15 April 2008
- 年：2008
- 卷：18
- 期：8
- 页码：2679-2683
- 全文大小：251 K
文摘
A novel bifunctional maleimido CHX-A″ DTPA chelator <strong>5strong> was developed and conjugated to the monoclonal antibody trastuzumab (Herceptin) and subsequently radiolabeled with <sup>111sup>In. The resulting <sup>111sup>In labeled immunoconjugate <strong>2strong> was demonstrated to bind to SKOV-3 ovarian cancer cells comparably to an isothiocyanato CHX-A″ DTPA modified native trastuzumab, <strong>1strong>. Through efficient thiol-maleimide chemistry, antibodies, peptides or other targeting vectors can now be modified with an established radioactive metal chelating agent CHX-A″ DTPA for imaging and/or therapies of cancer.