IUCr journals

Crystal-contact engineering to obtain a crystal form of the Kelch domain of human Keap1 suitable for ligand-soaking experiments

Acta Cryst. (2013). F69, 592-596 (http://doi.org/mvc)

[Keap1 image]

Keap1 is a substrate adaptor protein for a Cul3-dependent ubiquitin ligase complex and plays an important role in the cellular response to oxidative stress. It binds Nrf2 with its Kelch domain. The article describes the generation of a new crystal form of Keap1 which is suitable for ligand-soaking experiments. This makes possible the rapid generation of structures of Keap1 in complex with ligands, thus enabling rational design of Keap1-binding compounds.

S. Hörer, D. Reinert, K. Ostmann, Y. Hoevels and H. Nar