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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2014, Vol. 19 ›› Issue (1): 74-81.

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Advances in the study of post-transplantation diabetes mellitus resulting from tacrolimus via calcineurin/NFAT signaling

WANG Jiang-lin1,2, ZUO Xiao-cong1,2, YANG Meng1,2, ZHOU Ling-yun1,2   

  1. 1School of Pharmaceutical Sciences, Central South University, Changsha 410013, Hunan, China;
    2Department of Pharmacy, the Third Xiangya Hospital of Central South University, Changsha 410013, Hunan, China
  • Received:2013-03-21 Revised:2014-01-07 Online:2014-01-27 Published:2014-02-12

Abstract: Tacrolimus (FK506), a calcineurin phosphatase inhibitor, is the base anti-rejection drug after organ transplantation. Post-transplant diabetes mellitus (PTDM) is a complication after a solid organ transplant, and its incidence is widely variable, ranging from 2% to 53%. Tacrolimus is an important risk of PTDM. Tacrolimus inhibits the dephosphorylation of the nuclear factor of activated T-cells (NFATc) in cytoplasm by inhibiting the function of the calcineurin. Then the transport of NFATc into the nucleus and combination with the target DNA are impaired. As a consequence, the promoter cannot activate the transcription of related genes, which decrease the level of insulin by affecting beta cell proliferation, apoptosis and the secretion of insulin and increase the insulin resistance in the target tissue of insulin, leading to the development of PTDM.

Key words: Tacrolimus, Diabetes, Calcineurin/NFATc signaling

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