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Target intelligence / Profile preview
DNA Minor Groove Cross-Linking Agent (Pyrrolobenzodiazepine Dimer)
- Molecular classification
- DNA-interactive agent, Alkylating agent, Cross-linking agent
01
Overview
Pyrrolobenzodiazepine (PBD) dimers are a class of highly potent, sequence-selective DNA cross-linking agents that bind within the minor groove of DNA. These molecules form covalent interstrand cross-links, primarily at guanine bases, disrupting DNA replication and transcription. They are utilized as cytotoxic payloads in antibody-drug conjugates (ADCs) and as stand-alone antitumor agents due to their potent cytotoxic effects, even against resistant tumor cells.
- Other names
- PBD dimerPyrrolobenzodiazepine dimer
02
Mechanism of action
Sequence-selective interstrand covalent cross-linking of DNA via minor groove binding, leading to replication and transcription inhibition.
03
Biological functions
DNA replication inhibitionTranscription inhibitionApoptosis induction
04
Disease associations
Cancer
05
Safety considerations
CytotoxicityPotential for off-target effectsDevelopment of resistance
06
Interacting drugs
SJG-136
3 more in the full profile.
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