March 22, 2012
We've almost gotten used to GPCR structure publications - but today I'm seeing two publications in Nature that ought to rock the world of GPCR structural biology: morphine receptors. Structures of antagonist bound µ-opioid receptor and κ-opioid receptor with bound antagonist. The impact of these structures can not be underestimated since these structures give insight into the most used (and abused) clinical drugs and their workings on an atom scale. In a nutshell, these structures connect atom scale molecular structure to human behavior.
Manglik, A., Kruse, A., Kobilka, T., Thian, F., Mathiesen, J., Sunahara, R., Pardo, L., Weis, W., Kobilka, B., & Granier, S. (2012). Crystal structure of the µ-opioid receptor bound to a morphinan antagonist Nature DOI: 10.1038/nature10954
Wu, H., Wacker, D., Mileni, M., Katritch, V., Han, G., Vardy, E., Liu, W., Thompson, A., Huang, X., Carroll, F., Mascarella, S., Westkaemper, R., Mosier, P., Roth, B., Cherezov, V., & Stevens, R. (2012). Structure of the human κ-opioid receptor in complex with JDTic Nature DOI: 10.1038/nature10939
Congratulations to the Kobilka and the Stevens teams!