Abstract
The transcription factor ΔFosB accumulates in response to chronic insults such as drugs of abuse, L-3,4-dihydroxyphenylalanine (L-DOPA) or stress in specific regions of the brain, triggering long lasting neural and behavioral changes that underlie aspects of drug addiction, dyskinesia, and depression. Thus, small molecule chemical probes are urgently needed to investigate biological functions of ΔFosB. Herein we describe the identification of a novel phenanthridine analogue ZL0220 (27) as an active and promising ΔFosB chemical probe with micromolar inhibitory activities against ΔFosB homodimers and ΔFosB/JunD heterodimers.
Original language | English (US) |
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Article number | 127300 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 30 |
Issue number | 16 |
DOIs | |
State | Published - Aug 15 2020 |
Keywords
- Chemical probes
- Fluorescence polarization assay
- High-throughput screening
- ΔFosB homodimer
- ΔFosB/JunD heterodimer
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry