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Discovery of phenanthridine analogues as novel chemical probes disrupting the binding of DNA to ΔFosB homodimers and ΔFosB/JunD heterodimers.
Li, Yi; Liu, Zhiqing; Aglyamova, Galina; Chen, Jianping; Chen, Haiying; Bhandari, Mukund; White, Mark A; Rudenko, Gabrielle; Zhou, Jia.
Afiliación
  • Li Y; Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
  • Liu Z; Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
  • Aglyamova G; Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
  • Chen J; Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
  • Chen H; Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
  • Bhandari M; Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States.
  • White MA; Department of Biochemistry and Molecular Biology, University of Texas Medical Branch, Galveston, TX 77555, United States; Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch, Galveston, TX 77555, United States.
  • Rudenko G; Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States; Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch, Galveston, TX 77555, United States. Electronic address: garudenk@utmb.edu.
  • Zhou J; Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, United States; Sealy Center for Structural Biology and Molecular Biophysics, University of Texas Medical Branch, Galveston, TX 77555, United States. Electronic address: jizhou@utmb.edu.
Bioorg Med Chem Lett ; 30(16): 127300, 2020 08 15.
Article en En | MEDLINE | ID: mdl-32631520
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Fenantridinas / ADN / Proteínas Proto-Oncogénicas c-jun / Proteínas Proto-Oncogénicas c-fos / Descubrimiento de Drogas Tipo de estudio: Prognostic_studies Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Fenantridinas / ADN / Proteínas Proto-Oncogénicas c-jun / Proteínas Proto-Oncogénicas c-fos / Descubrimiento de Drogas Tipo de estudio: Prognostic_studies Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2020 Tipo del documento: Article País de afiliación: Estados Unidos Pais de publicación: Reino Unido