Enabling structure-based drug design of Tyk2 through co-crystallization with a stabilizing aminoindazole inhibitor.
Argiriadi, M.A., Goedken, E.R., Banach, D., Borhani, D.W., Burchat, A., Dixon, R.W., Marcotte, D., Overmeyer, G., Pivorunas, V., Sadhukhan, R., Sousa, S., Moore, N.S., Tomlinson, M., Voss, J., Wang, L., Wishart, N., Woller, K., Talanian, R.V.(2012) BMC Struct Biol 12: 22-22
- PubMed: 22995073 
- DOI: https://doi.org/10.1186/1472-6807-12-22
- Primary Citation of Related Structures:  
4E1Z, 4E20 - PubMed Abstract: 
Structure-based drug design (SBDD) can accelerate inhibitor lead design and optimization, and efficient methods including protein purification, characterization, crystallization, and high-resolution diffraction are all needed for rapid, iterative structure determination. Janus kinases are important targets that are amenable to structure-based drug design. Here we present the first mouse Tyk2 crystal structures, which are complexed to 3-aminoindazole compounds.
Organizational Affiliation: 
Department of Molecular & Cellular Pharmacology, Abbott Laboratories, Worcester, MA, USA. maria.argiriadi@abbott.com