RIKEN Center for Life Science Technologies

Topics

  • Research

    Latest publications from CLST.
     
  • News

    Awards, agreements, and other news.
  • Events

    Upcoming and past events including seminars, symposiums, open days.

For Public

To let you know about our research, this area contains 4 types of information about CLST; “Article”, “Videos”, “Event” and “Study”.
At “Article”, you can read articles on interviews and lectures, and you can enjoy the videos about CLST at “Videos”. If you want to meet and talk directly with the researcher, “Visit” give you some information of such events. You can find more difficult contents to know about our research deeply at “Study”.
  • Article
  • Event
  • Videos
  • Study

RESEARCH

New method of kinase crystal identification using fluorescent ligand

The RIKEN Center for Life Science Technologies has developed a new process that makes it easier to identify kinase crystals and screen new kinase inhibitors.

The small kinase inhibitor SKF86002 lacks intrinsic fluorescence, but becomes fluorescent upon binding to the ATP-binding sites of a wide variety of kinases. The co-crystals can be easily distinguished by their strong fluorescence (Figs. a, b). Moreover, the co-crystals lose their fluorescence when a compound, another kinase inhibitor, binds competitively and displaces the fluorescent SKF86002 (Figs. c, d).

This inhibitor can be a useful crystal marker, crystal stabilizer, and marker for screening new kinase inhibitors and identifying the ligand co-crystals for structural analysis. The information gained from the crystal structures of these soaked complexes can be used for structure-guided drug design studies.

The study was partly supported by the "Targeted Protein Research Program" of the Ministry of Education, Culture, Sports, Science and Technology, Japan. It was published in the journal Acta Crystallographica Section D (2014).

kinase.png

Related labs