Crystallization of Human Receptors

Takeshi Murata

Crystallization Group, Iwata Human Receptor Crystallography Project, ERATO, Japan Science and Technology Agency, Kyoto 606-8501, Japan

Although more than 50% of commercially available drugs target membrane proteins, most notably G-protein coupled receptors (GPCRs), structural studies of these membrane proteins have not been progressed very well due to the following three bottlenecks:

  • (1) They are difficult to over express and purify.
  • (2) They are difficult to crystallize because of their hydrophobicity.
  • (3) That in turn makes it difficult to obtain good X ray diffraction data.
My group focuses on second bottleneck. Our approach is to design binders which bind to these receptors, and increase hydrophilicity and crystallizabillity, and to develop effective crystallization methods for membrane proteins. In my talk, I would like to discuss the strategy to crystallize GPCRs.