DNA Double-Strand Break Induction via PBD-Dimer Payload (PBD-Dimer Payload)

PBD-dimers are potent DNA crosslinking agents used as payloads in antibody-drug conjugates (ADCs) to induce DNA double-strand breaks (DSBs) specifically in tumor cells. They bind to the minor groove of DNA and form covalent interstrand crosslinks, blocking replication and transcription. This leads to DSB formation and ultimately apoptosis. The selectivity of this approach is achieved through antibody targeting of tumor-specific antigens.

Other names

Pyrrolobenzodiazepine DimerPBD Interstrand Crosslinker

Covalent interstrand crosslink formation at guanine bases via minor groove binding, leading to replication blockade and double-strand breaks.