Evans Blue is an inhibitor of nuclear factor-kappa B (NF-kappa B)-DNA binding

• Tipo: Artigo em Revista Científica Internacional
• Data: 2004

Autores

Sharma, RK (Autor) Outra; Otsuka, M (Autor) Outra; Pande, V (Autor) Outra; Inoue, J (Autor) Outra; Ramos, MJ (Autor) FCUP

Revista

Título: Bioorganic and Medicinal Chemistry Letters

Vol. 14

Páginas: 6123-6127

ISSN: 0960-894X

Editora: Elsevier

Indexação

ISI Web of Knowledge - 14 Citações

Scopus - 16 Citações

Classificação Científica

FOS: Ciências exactas e naturais > Química

Outras Informações

ID Authenticus: P-000-79X

DOI: 10.1016/j.bmcl.2004.07.096

Abstract (EN): Nuclear factor-kappa B (NF-KB) is an important transcription factor, involved in many immune and inflammatory responses. It is critical in HIV gene expression as it has kappa B binding sites in the HIV-1 long-terminal repeat. Hence, targeting NF-KB to prevent its DNA binding holds a significant therapeutic potential. In this context, we report Evans Blue as a novel inhibitor of NF-kappaB-DNA binding. Evans Blue was found to be inhibiting DNA binding of NF-KB at a low concentration of 100 PM. Further, molecular modeling studies using docking and generation of electrostatic potential maps predicted a possible binding mode of EB to the DNA binding region of NF-kappaB, consistent with the experimental activity.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 5