674774-66-4

Upstream product

• 113854-62-9 1-[1-(p-toluenesulfonyl)indol-4-yloxy]-2,3-epoxypropane 
• 2380-94-1 1H-indol-4-ol 
• 15336-72-8 4,4'-bipiperidine 
• 674774-62-0 N-[3-(N-tosyl-4-indolyloxy)-2-hydroxypropyl]-N'-Boc-1,3-propanediamine 
• 674774-64-2 adamantan-1-yl-[4,4']bipiperidinyl-1-yl-methanone 
• 35308-87-3 4-(oxiranylmethoxy)-1H-indole 

Relevant academic research and scientific papers

SMALL MOLECULE INHIBITORS OF HER2 EXPRESSION

Peptide mimetic small molecule inhibitors of Sur-2 are provided having the general formula (I).

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 α-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.