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Drug Names(s): 1R-(E1)-(E1)
1R-(E1)-(E1) is a novel bispecific hexavalent antibody (HexAb) targeting IGF-1R/Trop-2. 1R-(E1)-(E1), comprising the full IgG of hR1 (humanized anti-IGF-1R) and four Fabs of hRS7 (humanized anti-Trop-2), was generated with Immunomedics' Dock-and-Lock (DNL) technology.
DNL utilizes the natural interaction between two proteins, cyclic AMP-dependent protein kinase, or PKA, and A-kinase anchoring proteins, or AKAPs. The region that is involved in such interaction for PKA is called the dimerization and docking domain, or DDD, which always appears in pairs. Its binding partner in AKAPs is the anchoring domain, or AD. When mixed together, DDD and AD will bind with each other spontaneously to form a binary complex, a process termed docking. Once “docked,” certain amino acid residues incorporated into DDD and AD will react with each other to “lock” them into a stably-tethered structure. The outcome of DNL is the exclusive generation of a stable complex, in a quantitative manner that retains the full biological activities of its individual components.
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