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Polyphenol Compound as a Transcription Factor Inhibitor.

Park S - Nutrients (2015)

Bottom Line: Although their mechanism of action is not fully defined, polyphenols including flavonoids were found to act mostly as site-directed small molecule inhibitors on signaling.There are many reports in the literature of screening initiatives suggesting improved drugs that can modulate the transcription factor interactions responsible for disease.In this review, we focus on polyphenol compound inhibitors against dimeric forms of transcription factor components of intracellular signaling pathways (for instance, c-jun/c-fos (Activator Protein-1; AP-1), c-myc/max, Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and β-catenin/T cell factor (Tcf)).

View Article: PubMed Central - PubMed

Affiliation: Department of Applied Chemistry, Dongduk Women's University, Seoul 136-714, Korea. sypark21@dongduk.ac.kr.

ABSTRACT
A target-based approach has been used to develop novel drugs in many therapeutic fields. In the final stage of intracellular signaling, transcription factor-DNA interactions are central to most biological processes and therefore represent a large and important class of targets for human therapeutics. Thus, we focused on the idea that the disruption of protein dimers and cognate DNA complexes could impair the transcriptional activation and cell transformation regulated by these proteins. Historically, natural products have been regarded as providing the primary leading compounds capable of modulating protein-protein or protein-DNA interactions. Although their mechanism of action is not fully defined, polyphenols including flavonoids were found to act mostly as site-directed small molecule inhibitors on signaling. There are many reports in the literature of screening initiatives suggesting improved drugs that can modulate the transcription factor interactions responsible for disease. In this review, we focus on polyphenol compound inhibitors against dimeric forms of transcription factor components of intracellular signaling pathways (for instance, c-jun/c-fos (Activator Protein-1; AP-1), c-myc/max, Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and β-catenin/T cell factor (Tcf)).

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Flavone and flavanone.
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nutrients-07-05445-f002: Flavone and flavanone.

Mentions: On the other hand, flavanone and flavonoids that include the same skeleton such as naringenin did not show inhibitory activity against β-catenin/Tcf and DNA binding, in discord with other types of flavonoids [68,71]. From the three dimensional structure, the 2-substituted B ring of flavanone seems to be puckered from the plane, with a different shape from the other flavone skeletons containing conjugated double bonds of C3 rings as shown in Figure 2. This puckered structure may be unfit to block β-catenin/Tcf and DNA complex formation.


Polyphenol Compound as a Transcription Factor Inhibitor.

Park S - Nutrients (2015)

Flavone and flavanone.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4663573&req=5

nutrients-07-05445-f002: Flavone and flavanone.
Mentions: On the other hand, flavanone and flavonoids that include the same skeleton such as naringenin did not show inhibitory activity against β-catenin/Tcf and DNA binding, in discord with other types of flavonoids [68,71]. From the three dimensional structure, the 2-substituted B ring of flavanone seems to be puckered from the plane, with a different shape from the other flavone skeletons containing conjugated double bonds of C3 rings as shown in Figure 2. This puckered structure may be unfit to block β-catenin/Tcf and DNA complex formation.

Bottom Line: Although their mechanism of action is not fully defined, polyphenols including flavonoids were found to act mostly as site-directed small molecule inhibitors on signaling.There are many reports in the literature of screening initiatives suggesting improved drugs that can modulate the transcription factor interactions responsible for disease.In this review, we focus on polyphenol compound inhibitors against dimeric forms of transcription factor components of intracellular signaling pathways (for instance, c-jun/c-fos (Activator Protein-1; AP-1), c-myc/max, Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and β-catenin/T cell factor (Tcf)).

View Article: PubMed Central - PubMed

Affiliation: Department of Applied Chemistry, Dongduk Women's University, Seoul 136-714, Korea. sypark21@dongduk.ac.kr.

ABSTRACT
A target-based approach has been used to develop novel drugs in many therapeutic fields. In the final stage of intracellular signaling, transcription factor-DNA interactions are central to most biological processes and therefore represent a large and important class of targets for human therapeutics. Thus, we focused on the idea that the disruption of protein dimers and cognate DNA complexes could impair the transcriptional activation and cell transformation regulated by these proteins. Historically, natural products have been regarded as providing the primary leading compounds capable of modulating protein-protein or protein-DNA interactions. Although their mechanism of action is not fully defined, polyphenols including flavonoids were found to act mostly as site-directed small molecule inhibitors on signaling. There are many reports in the literature of screening initiatives suggesting improved drugs that can modulate the transcription factor interactions responsible for disease. In this review, we focus on polyphenol compound inhibitors against dimeric forms of transcription factor components of intracellular signaling pathways (for instance, c-jun/c-fos (Activator Protein-1; AP-1), c-myc/max, Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and β-catenin/T cell factor (Tcf)).

Show MeSH
Related in: MedlinePlus