Chemistry and Biology of the Immunosuppressant(-)-FK-506.

FK 506: an effective immunosuppressant for islet xenotransplantation.

R EPLACING the damaged insulin-producing tissue by transplantation of pancreatic islets is considered the most physiological approach to diabetes treatment and has the potential to prevent the development of chronic complications. Due to the large number of potential diabetic recipients. it would be impossible to obtain sufficient supply of donor organs to fulfill the demands. One solution to r...

FK-506, a novel immunosuppressant isolated from a Streptomyces. II. Immunosuppressive effect of FK-506 in vitro.

The immuno-pharmacological profile of a novel immunosuppressive agent, FK-506 produced by a streptomycete, is presented here. We proceeded to test the effect of the agent on various in vitro immune systems. It showed that mixed lymphocyte reaction, cytotoxic T cell generation, the production of T cell-derived soluble mediators such as interleukin 2 (IL-2), interleukin 3 and gamma-interferon and...

Independent inhibition of calcineurin and K+ currents by the immunosuppressant FK-506 in rat ventricle.

FK-506 increases the cytosolic Ca2+ concentration transient in rat ventricular myocytes by prolonging the action potential through inhibition of the K+ currents I to and I K[ J. Physiol. (Lond.) 501: 509-516, 1997]. Physiological and biochemical techniques were used in parallel to examine the electrophysiological mechanisms and the role of calcineurin inhibition in these effects. FK-506 prolong...

Independent inhibition of calcineurin and K1 currents by the immunosuppressant FK-506 in rat ventricle

DuBell, W. H., S. T. Gaa, W. J. Lederer, and T. B. Rogers. Independent inhibition of calcineurin and K1 currents by the immunosuppressant FK-506 in rat ventricle. Am. J. Physiol. 275 (Heart Circ. Physiol. 44): H2041–H2052, 1998.—FK-506 increases the cytosolic Ca21 concentration transient in rat ventricular myocytes by prolonging the action potential through inhibition of the K1 currents Ito and...

Effect of the immunosuppressant FK 506 on insulin release from adult rat islets of Langerhans.