adamanolol has been researched along with wrenchnolol* in 2 studies
1 review(s) available for adamanolol and wrenchnolol
| Article | Year |
|---|---|
Small organic molecules that modulate gene transcription.
Regulation of gene expression by transcription factors touches all aspects of human biology and often induces extreme phenotypes. Its external, precise control by small organic molecules represents a challenge in chemistry and biology. Here, we summarize recent progress in the field, together with contributions from our laboratory. Small-molecule modulators of transcription, including small-molecule transcription factors could find their use in basic biological studies and therapeutic intervention. Topics: Adamantane; Animals; Antineoplastic Agents; Drug Design; Humans; Indoles; Molecular Structure; Protein Conformation; Transcription Factors; Transcription, Genetic | 2006 |
1 other study(ies) available for adamanolol and wrenchnolol
| Article | Year |
|---|---|
A wrench-shaped synthetic molecule that modulates a transcription factor-coactivator interaction.
Development of synthetic molecules that provide external control over the transcription of a given gene represents a challenge in medicinal and bioorganic chemistry. Here we report design and analysis of wrenchnolol, a wrench-shaped synthetic molecule that impairs the transcription of the Her2 oncogene by disrupting association of transcription factor ESX with its coactivator Sur-2. The "jaw" part of the compound mimics the alpha-helical interface of the activation domain of ESX, and the "handle" region accepts chemical modifications for a range of analysis. A water-soluble handle permitted NMR study in aqueous solution; a biotinylated handle verified the selectivity of the interaction, and a fluorescent handle confirmed the cell permeability of the compound. The case study of wrenchnolol foreshadows the promise and the challenge of targeting protein-protein interactions in the nucleus and may lead to the development of unique synthetic modulators of gene transcription. Topics: Adamantane; Biomimetic Materials; Bridged-Ring Compounds; Cell Line, Tumor; DNA-Binding Proteins; Fluorescein; Genes, erbB-2; Humans; Indoles; Mediator Complex; Models, Molecular; Propanols; Proto-Oncogene Proteins; Proto-Oncogene Proteins c-ets; Receptor, ErbB-2; Structure-Activity Relationship; Trans-Activators; Transcription Factors; Transcriptional Activation | 2004 |