The first Hes1 dimer inhibitors from natural products.
Basic Information
ID: ALA1156024
Journal: Bioorg Med Chem Lett
Title: The first Hes1 dimer inhibitors from natural products.
Authors: Arai MA, Masada A, Ohtsuka T, Kageyama R, Ishibashi M.
Abstract: In the present study, we developed a high-throughput screening system for small molecule-inhibitors of the basic helix-loop-helix (bHLH) transcriptional repressor factor Hes1. Successful dimerization of Hes1 immobilized on a microplate and fluorophore (Cy3)-labelled Hes1 was confirmed. Using this system, several natural products were identified as the first Hes1 dimer inhibitors. Of these, two compounds which were isolated from myxomycetes (true slime molds) inhibited Hes1 from N box-dependent suppression of the gene expression in C3H10T1/2 cells.
CiteXplore: 19716294
DOI: 10.1016/j.bmcl.2009.07.146
Patent ID: ┄