β-Lactam-based approach for the chemical programming of aldolase antibody 38C2

JI Gavrilyuk, U Wuellner, CF Barbas

文献索引：Gavrilyuk, Julia I.; Wuellner, Ulrich; Barbas III, Carlos F. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 5 p. 1421 - 1424

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被引用次数: 27

摘要

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 ...