Beta-lactam-based approach for the chemical programming of aldolase antibody 38C2.
Beta-lactam-based approach for the chemical programming of aldolase antibody 38C2.
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DOI：
10.1016/j.bmcl.2009.01.028
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发表时间：
2009-03-01
影响因子：
2.7
通讯作者：
Barbas CF 3rd
中科院分区：
文献类型：
--
作者：
Gavrilyuk JI;Wuellner U;Barbas CF 3rd
Irreversible chemical programming of monoclonal aldolase antibody (mAb) 38C2 has been accomplished with β-lactam equipped targeting modules. A model study was first performed with β-lactam conjugated to biotin. This conjugate efficiently and selectively modified the catalytic site lysine (LysH93) of mAb 38C2. We then conjugated a β-lactam to a cyclic-RGD peptide to chemically program mAb 38C2 to target integrin receptors αvβ3 and αvβ5. 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.
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