Edited by: Karen Young Kreeger
J.P. Griffith, J.L. Kim, E.E. Kim, M.D. Sintchak, J.A. Thomson, M.J. Fitzgibbon, M.A. Fleming, P.R. Caron, K. Hsiao, M.A. Navia, "X-ray structure of calcineurin inhibited by the immunophilin-immunosuppressant FKBP12-FK506 complex," Cell, 82:507-22, 1995. (Cited in close to 70 publications as of February 1997)
FK506 is an immunosuppressant drug used for preventing graft rejection after organ transplantation and for treating some autoimmune diseases. The drug works by inhibiting the action of the enzyme calcineurin and its associated cellular binding protein, FKBP12. FK506 and FKBP12 form a molecular complex that suppresses T-cell activation by binding to calcineurin and inhibiting its phosphatase activity.
'FULL-SERVICE' COMPLEX: Vertex researchers Jim Griffith, left, and Joseph Kim described the structure of a large, multicomponent immunosuppressant molecular complex. "This paper provides the structural basis for understanding calcineurin inhibition by the FKBP12-FK506 complex," says Joseph Kim, a staff scientist at Cambridge, Mass.-based Vertex Pharmaceuticals ...
