X-ray structure of calcineurin inhibited by the immunophilin-immunosuppressant FKBP12-FK506 complex

@article{Griffith1995XraySO,
  title={X-ray structure of calcineurin inhibited by the immunophilin-immunosuppressant FKBP12-FK506 complex},
  author={J. P. Griffith and J. Kim and E. Kim and M. Sintchak and J. Thomson and M. Fitzgibbon and Mark A. Fleming and P. Caron and K. Hsiao and M. Navia},
  journal={Cell},
  year={1995},
  volume={82},
  pages={507-522}
}
  • J. P. Griffith, J. Kim, +7 authors M. Navia
  • Published 1995
  • Biology, Medicine
  • Cell
  • The X-ray structure of the ternary complex of a calcineurin A fragment, calcineurin B, FKBP12, and the immunosuppressant drug FK506 (also known as tacrolimus) has been determined at 2.5 A resolution, providing a description of how FK506 functions at the atomic level. In the structure, the FKBP12-FK506 binary complex does not contact the phosphatase active site on calcineurin A that is more than 10 A removed. Instead, FKBP12-FK506 is so positioned that it can inhibit the dephosphorylation of its… CONTINUE READING
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