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钙调神经磷酸酶调节亚基对新型隐球菌的毒力至关重要,并介导其与FKBP12-FK506的相互作用。

Calcineurin regulatory subunit is essential for virulence and mediates interactions with FKBP12-FK506 in Cryptococcus neoformans.

作者信息

Fox D S, Cruz M C, Sia R A, Ke H, Cox G M, Cardenas M E, Heitman J

机构信息

Department of Genetics, 322 CARL Bldg., Box 3546, Duke University Medical Center, Research Drive, Durham, NC 27710, USA.

出版信息

Mol Microbiol. 2001 Feb;39(4):835-49. doi: 10.1046/j.1365-2958.2001.02295.x.

Abstract

Calcineurin is a Ca2+-calmodulin-regulated protein phosphatase that is the target of the immunosuppressive drugs cyclosporin A and FK506. Calcineurin is a heterodimer composed of a catalytic A and a regulatory B subunit. In previous studies, the calcineurin A homologue was identified and shown to be required for growth at 37 degrees C and hence for virulence of the pathogenic fungus Cryptococcus neoformans. Here, we identify the gene encoding the calcineurin B regulatory subunit and demonstrate that calcineurin B is also required for growth at elevated temperature and virulence. We show that the FKR1-1 mutation, which confers dominant FK506 resistance, results from a 6 bp duplication generating a two-amino-acid insertion in the latch region of calcineurin B. This mutation was found to reduce FKBP12-FK506 binding to calcineurin both in vivo and in vitro. Molecular modelling based on the FKBP12-FK506-calcineurin crystal structure illustrates how this mutation perturbs drug interactions with the phosphatase target. In summary, our studies reveal a central role for calcineurin B in virulence and antifungal drug action in the human fungal pathogen C. neoformans.

摘要

钙调神经磷酸酶是一种受Ca2+ -钙调蛋白调节的蛋白磷酸酶,是免疫抑制药物环孢菌素A和FK506的作用靶点。钙调神经磷酸酶是一种异二聚体,由催化性A亚基和调节性B亚基组成。在先前的研究中,已鉴定出钙调神经磷酸酶A的同源物,并表明其对于在37摄氏度下生长是必需的,因此对于致病真菌新生隐球菌的毒力也是必需的。在此,我们鉴定了编码钙调神经磷酸酶B调节亚基的基因,并证明钙调神经磷酸酶B对于在高温下生长和毒力也是必需的。我们表明,赋予显性FK506抗性的FKR1 - 1突变是由一个6 bp的重复导致的,该重复在钙调神经磷酸酶B的闩锁区域产生了一个双氨基酸插入。发现该突变在体内和体外均降低了FKBP12 - FK506与钙调神经磷酸酶的结合。基于FKBP12 - FK506 -钙调神经磷酸酶晶体结构的分子建模说明了该突变如何扰乱药物与磷酸酶靶点的相互作用。总之,我们的研究揭示了钙调神经磷酸酶B在人类真菌病原体新生隐球菌的毒力和抗真菌药物作用中的核心作用。

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