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• W1975891149 abstract "Annals of the New York Academy of SciencesVolume 685, Issue 1 p. 22-36 FK-506–A Novel Immunosuppressant WILLIAM H. PARSONS, WILLIAM H. PARSONS Departments of Basic Medicinal Chemistry and Immunology Merck Research Laboratories P.O. Box 2000 Rahway, New Jersey 07065Search for more papers by this authorNOLAN H. SIGAL, NOLAN H. SIGAL Departments of Basic Medicinal Chemistry and Immunology Merck Research Laboratories P.O. Box 2000 Rahway, New Jersey 07065Search for more papers by this authorMATTHEW J. WYVRATT, MATTHEW J. WYVRATT Departments of Basic Medicinal Chemistry and Immunology Merck Research Laboratories P.O. Box 2000 Rahway, New Jersey 07065Search for more papers by this author WILLIAM H. PARSONS, WILLIAM H. PARSONS Departments of Basic Medicinal Chemistry and Immunology Merck Research Laboratories P.O. Box 2000 Rahway, New Jersey 07065Search for more papers by this authorNOLAN H. SIGAL, NOLAN H. SIGAL Departments of Basic Medicinal Chemistry and Immunology Merck Research Laboratories P.O. Box 2000 Rahway, New Jersey 07065Search for more papers by this authorMATTHEW J. WYVRATT, MATTHEW J. WYVRATT Departments of Basic Medicinal Chemistry and Immunology Merck Research Laboratories P.O. Box 2000 Rahway, New Jersey 07065Search for more papers by this author First published: June 1993 https://doi.org/10.1111/j.1749-6632.1993.tb35847.xCitations: 39AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL References 1 Borel, J. F., C. Feurer, H. U. Gubler & H. Stahelin. 1976. 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J. Siekierka, J. Chin & N. I. Hutchinson. 1989. The immunosup-pressant FK-506 selectively inhibits expression of early T cell activation genes. J. Immunol. 143: 718– 726. 26 Granelli-piperno, A., P. Nolan, K. Inaba & R. M. Steinman. 1990. The effect of immunosuppressive agents on the induction of nuclear factors that bind to sites on the interleukin 2 promotor. J. Exp. Med. 172: 1869– 1872. 27 Dumont, F. J., M. J. Staruch, S. L. Koprak, M. R. Melino & N. H. Sigal. 1990. Distinct mechanisms of suppression of murine T cell activation by the related macrolides FK-506 and rapamycin. J. Immunol. 144: 251– 258. 28 Dumont, F. J., M. R. Melino, M. J. Staruch, S. L. Koprak, P. A. Fischer & N. H. Sigal. 1990. The immunosuppressive macrolides FK-506 and rapamycin act as reciprocal antagonists in murine T cells. J. Immunol. 144: 1418– 1424. 29 Siekierka, J. J., S. H. Hung, M. Poe, C. S. Lin & N. H. Sigal. 1989. A cytosolic binding protein for the immunosuppressant FK-506 has peptidyl-prolyl isomerase activity but is distinct from cyclophilin. Nature 341: 755– 757. 30 Fretz, H., M. W. Albers, A. Galat, R. F. Standaert, W. S. Lane, S. J. Burakoff, B. E. Bierer & S. L. Schreiber. 1991. Rapamycin and FK-506 binding proteins (Immunophilins). J. Am. Chem. Soc. 113: 1409– 1411. 31 Bierer, B. E., P. S. Mattila, R. F. Standaert, L. A. Herzenberg, S. J. Burakoff, G. Crabtree & S. L. Schreiber. 1990. Two distinct signal transmission pathways in T lymphocytes are inhibited by complexes formed between an immunophilin and either FK-506 or rapamycin. Proc. Natl. Acad. Sci. 87: 9231– 9235. 32 Sigal, N. H., F. Dumont, P. Durette, J. J. Siekierka, L. Peterson, D. H. Rich, M. J. Staruch, M. R. Melino, S. L. Koprak, D. Williams, B. Witzel & J. M. Pisano. 1991. Is cyclophilin involved in the immunosuppressive and nephrotoxic mechanism of action of cyclopsorin A?. J. Exp. Med. 173: 619– 628. 33 Liu, J., J. D. Farmer, W. S. Lane, J. Friedman, I. Weissman & S. L. Schrieber. 1991. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK-506 complexes. Cell. 66: 807– 815. 34 Dumont, F. J., M. J. Staruch, S. L. Koprak, J. J. Siekierka, C. S. Lin, R. Harrison, T. Sewell, V. M. Kindt, T. R. Beattie, M. Wyvratt & N. H. Sigal. 1992. The immunosuppressive and toxic effects of FK-506 are mechanistically related: Pharmacology of a novel antagonist of FK-506 and rapamycin. J. Exp. Med. 176: 751– 760. 35 Fruman, D. A., C. B. Klee, B. E. Bierer & S. J. Burakoff. 1992. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK-506 and cyclosporin A. Proc. Natl. Acad. Sci. USA 89: 3686– 3690. 36 O'keefe, S. J., J. Tamura, R. L. Kinkaid, M. J. Tocci & E. A. O'Neill. 1992. FK-506– and CsA-sensitive activation of the interleukin-2 promoter by calcineurin. Nature 357: 692– 694. 37 Clipstone, N. A. & G. R. Crabtree. 1992. Identification of calcineurin as a key signalling enzyme in lymphocyte-T activation. Nature 357: 695– 697. 38 Van Duyne, G. D., R. F. Standaert, P. A. Karplus, S. L. Schreiber & J. Clardy. 1991. Atomic structure of FKBP-FK-506, an immunophilin-immunosuppressant complex. Science 252: 839– 842. 39 Becker, J. W., J. Rotonda, B. M. Mckeever, K. Chan, A. I. Marcy, G. Wiederrecht, J. D. Hermes & J. P. Springer. 1993. FK-506–binding protein: Three-dimensional structure of the complex with the antagonist L-685,818. J. Biol. Chem. In press. 40 Rotonda, J. & J. W. Becker. 1991. The three-dimensional structure of the yeast FK-506–binding protein complex with FK-506. American Crystallographic Association Annual Meeting, abstract PB36. 41 Mckeever, B. M., J. Rotonda & J. W. Becker. 1991. Three-dimensional structure of the drug-free FK-506 binding protein. American Crystallographic Association Annual Meeting, abstract PB38. 42 Moore, J. M., D. A. Peattie, M. J. Fitzgibbon & J. A. Thomson. 1991. Solution structure of the major binding protein for the immunosuppressant FK-506. Nature 351: 248– 250. 43 Michnick, S. W., M. K. Rosen, T. J. Wandless, M. Karplus & S. L. Schreiber. 1991. Solution structure of FKBP, a rotamase enzyme and receptor for FK506 and rapamycin. Science 252: 836– 839. 44 Becker, J. W. Unpublished results. 45 Karuso, P., H. Kessler & D. F. Mierke. 1990. Solution structure of FK-506 from nuclear magnetic resonance and molecular dynamics. J. Am. Chem. Soc. 112: 9434– 9436. 46 Taga, T., H. Tanaka, T. Goto & S. Tada. 1987. Structure of a new macrocyclic antibiotic. Acta Crystallogr. C43: 751– 753. 47 Aldape, R. A., O. Futer, M. T. Decenzo, B. P. Jarrett, M. A. Murcko & D. J. Livingston. 1992. Charged surface residues of FKBP12 participate in formation of the FKBP12–FK-506–calcineurin complex. J. Biol. Chem. 267: 16029– 16032. 48 Armitage, J. M., R. L. Kormos, S. Morita, J. Fung, G. C. Marrone, R. L. Hardesty, B. P. Griffith & T. E. Starzl. 1992. Critical trial of FK-506 immunosuppression in adult cardiac transplantation. Ann. Thorac. Surg. 54: 205– 211. 49 Ochiai, T., M. Nagata, K. Nakajima, T. Suzuki, K. Sakamoto, K. Enomoto, Y. Gunji, T. Uematsu, T. Goto, S. Hori, T. Kenmochi, T. Nakagouri, T. Asano, K. Isono, K. Hamaguchi, H. Tuchida, K. Nakahara, N. Inamura & T. Goto. 1987. Studies of the effects of FK-506 on renal allografting in the beagle dog. Transplantation 44 (6): 729– 733. 50 Kumano, K., G. Wang, T. Endo & S. Kuwao. 1991. FK-506–induced nephrotoxicity in rats. Transplant. Proc. 23: 512– 515. Citing Literature Volume685, Issue1Immunomodulating DrugsJune 1993Pages 22-36 ReferencesRelatedInformation" @default.
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