Literature DB >> 15546742

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

Rakesh K Sharma1, Masami Otsuka, Vineet Pande, Jun-ichiro Inoue, Maria João Ramos.   

Abstract

Nuclear factor-kappa B (NF-kappaB) 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-kappaB 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-kappaB at a low concentration of 100 microM. 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.

Entities:  

Mesh:

Substances:

Year:  2004        PMID: 15546742     DOI: 10.1016/j.bmcl.2004.07.096

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Docking of molecules identified in bioactive medicinal plants extracts into the p50 NF-kappaB transcription factor: correlation with inhibition of NF-kappaB/DNA interactions and inhibitory effects on IL-8 gene expression.

Authors:  Laura Piccagli; Enrica Fabbri; Monica Borgatti; Valentino Bezzerri; Irene Mancini; Elena Nicolis; Maria C Dechecchi; Ilaria Lampronti; Giulio Cabrini; Roberto Gambari
Journal:  BMC Struct Biol       Date:  2008-09-03

2.  DSE-FRET: A new anticancer drug screening assay for DNA binding proteins.

Authors:  Toru Miyagi; Bunsyo Shiotani; Ryuya Miyoshi; Takuya Yamamoto; Takanori Oka; Kazuo Umezawa; Takahiro Ochiya; Mikihisa Takano; Hidetoshi Tahara
Journal:  Cancer Sci       Date:  2014-05-14       Impact factor: 6.716

  2 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.