Drug intelligence / Profile preview

netropsin

Development stage
Preclinical
Lead developer
Florida International University
Modality
Small Molecules
Administration
Parenteral
01

Overview

Netropsin is a pyrrole-amidine natural product antibiotic originally isolated from *Streptomyces netropsis*. It is a classic example of a DNA minor groove binder, exhibiting high affinity for AT-rich sequences. By occupying the minor groove, netropsin physically blocks the binding of various DNA-binding proteins, including the High-mobility group AT-hook 2 (HMGA2) transcription factor. Research indicates that by inhibiting HMGA2-DNA interactions, netropsin can suppress the epithelial-mesenchymal transition (EMT) in melanoma cells, particularly those with BRAF mutations, thereby reducing metastasis and migratory behavior. Although it possesses potent antibacterial and antiviral activities, its clinical utility has been limited by systemic toxicity, and it is currently utilized primarily as a biochemical research tool for studying DNA-protein interactions and as a lead compound for developing sequence-specific DNA binders.

Other names
congocidinesinanomycin
02

Targets

AT-rich double-stranded B-form DNAHigh-mobility group AT-hook 2–DNA complex

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