Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 30, Issue 16, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127300
Keywords
Delta FosB homodimer; Delta FosB/JunD heterodimer; Chemical probes; High-throughput screening; Fluorescence polarization assay
Categories
Funding
- NIH/NIDA [R01 DA040621]
- John D. Stobo, M.D. Distinguished Chair Endowment Fund at UTMB
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The transcription factor Delta FosB 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 Delta FosB. Herein we describe the identification of a novel phenanthridine analogue ZL0220 (27) as an active and promising Delta FosB chemical probe with micromolar inhibitory activities against Delta FosB homodimers and Delta FosB/JunD heterodimers.
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