Analogs of the Dopamine Metabolite 5,6-Dihydroxyindole Bind Directly to and Activate the Nuclear Receptor Nurr1.

The nuclear receptor-related 1 protein, Nurr1, is a transcription factor critical for the development and maintenance of dopamine-producing neurons in the substantia nigra pars compacta, a cell population that progressively loses the ability to make dopamine and degenerates in Parkinson's disease. Recently, we demonstrated that Nurr1 binds directly to and is regulated by the endogenous dopamine metabolite 5,6-dihydroxyindole (DHI). Unfortunately, DHI is an unstable compound, and thus a poor tool for studying Nurr1 function.

Simple and Efficient Preparation of O- and S-GlcNAcylated Amino Acids through InBr-Catalyzed Synthesis of β- N-Acetylglycosides from Commercially Available Reagents.

The facile synthesis of serine, threonine, and cysteine β-glycosides using commercially available peracetylated β- N-acetylglucosamine (β-AcGlcNAc) and catalytic amounts of indium bromide (InBr) is described. This method involves only inexpensive reagents that require no further modification or special handling. The reagents are simply mixed, dissolved, and refluxed to afford the GlcNAcylated amino acids in great yields (70-80%).