HNF4α - role in drug metabolism and potential drug target?

Hepatocyte nuclear factor 4 alpha (HNF4 alpha) is a highly conserved member of the nuclear receptor superfamily of ligand-dependent transcription factors It is best known as a master regulator of liver-specific gene expression, especially those genes involved in lipid transport and glucose metabolism However there is also a growing body of work that indicates the importance of HNF4 alpha in the regulation of genes involved in xenobiotic and drug metabolism A recent study identifying the essential fatty acid linoleic acid (LA, C18 2) as the endogenous reversible ligand for HNF4 alpha suggests that HNF4 alpha may also be a potential drug target and that its activity may be regulated by diet This review will discuss the role of HNF4 alpha in drug metabolism including the genes it regulates, the factors that regulate its activity and its potential as a drug target