Immunosuppression complexes

Pharmacology Sirolimus, a macrolide immunosuppressive agent, inhibits both T-lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (interleukin-2, -4, and -15) stimulation and also inhibits antibody production. In cells, sirolimus binds to the immunophilin, FK binding protein-12 (FKBP-12), to generate an immunosuppressive complex. 

II. Inhibition by Immunophilin/Immunosuppressant Complexes The Presenting Protein Strategy... 

Van Duyne, G. D., Standaert, R. F., Karplus, P. A., Schreiber, S. L., and Clardy, J. (1991a). Atomic structure of FKBP-FK506, an immunophilin-immunosuppressant complex. 

X-ray structures have been published of the catalytic subunit of rabbit muscle PP-1 complexed with the polypeptide microcystin131 and of human PP-1 with tungstate.132 The X-ray structures are also available of free human calcineurin (Fig. 23), as well as of human and bovine brain calcineurin complexed with the immunosuppressant complex FKBP12/FK506, which does not contact the active site, but binds adjacent in a manner that hinders access.133,134 Calcineurin is involved in the... 

Atomic structure of FKBP-FK506, an immunophilin-immunosuppressant complex, Science 1991, 252, 839-842. 

Waag DM, Williams JC. Immune modulation by Coxiella burnetii Characterization of a Phase I immunosuppressive complex expressed among strains. Immunopharmacol Immunotoxicol. 1988 10 231-260. 

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