期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 5, 页码 1421-1424出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.01.028
关键词
Monoclonal antibody; Aldolase antibody; Chemically programmed antibody; Integrins
资金
- National Institutes of Health [RO1 CA104045]
Irreversible chemical programming of monoclonal aldolase antibody (mAb) 38C2 has been accomplished with beta-lactam-equipped targeting modules. A model study was first performed with beta-lactam conjugated to biotin. This conjugate efficiently and selectively modified the catalytic site lysine (LysH93) of mAb 38C2. We then conjugated a beta-lactam to a cyclic-RGD peptide to chemically program mAb 38C2 to target integrin receptors alpha(nu)beta(3) and alpha(nu)beta(5). The chemically programmed antibody bound specifically to the isolated integrin receptor proteins as well as the integrins expressed on human melanoma cells. This approach provides an efficient and versatile solution to irreversible chemical programming of aldolase antibodies. (C) 2009 Elsevier Ltd. All rights reserved.
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