Department of Pediatrics, Division of Pediatric Infectious Diseases, Duke University Medical Center, Durham, North Carolina, United States of America.
PLoS Pathog. 2013;9(8):e1003564. doi: 10.1371/journal.ppat.1003564. Epub 2013 Aug 22.
The fungus Aspergillus fumigatus is a leading infectious killer in immunocompromised patients. Calcineurin, a calmodulin (CaM)-dependent protein phosphatase comprised of calcineurin A (CnaA) and calcineurin B (CnaB) subunits, localizes at the hyphal tips and septa to direct A. fumigatus invasion and virulence. Here we identified a novel serine-proline rich region (SPRR) located between two conserved CnaA domains, the CnaB-binding helix and the CaM-binding domain, that is evolutionarily conserved and unique to filamentous fungi and also completely absent in human calcineurin. Phosphopeptide enrichment and tandem mass spectrometry revealed the phosphorylation of A. fumigatus CnaA in vivo at four clustered serine residues (S406, S408, S410 and S413) in the SPRR. Mutation of the SPRR serine residues to block phosphorylation led to significant hyphal growth and virulence defects, indicating the requirement of calcineurin phosphorylation at the SPRR for its activity and function. Complementation analyses of the A. fumigatus ΔcnaA strain with cnaA homologs from the pathogenic basidiomycete Cryptococcus neoformans, the pathogenic zygomycete Mucor circinelloides, the closely related filamentous fungi Neurospora crassa, and the plant pathogen Magnaporthe grisea, revealed filamentous fungal-specific phosphorylation of CnaA in the SPRR and SPRR homology-dependent restoration of hyphal growth. Surprisingly, circular dichroism studies revealed that, despite proximity to the CaM-binding domain of CnaA, phosphorylation of the SPRR does not alter protein folding following CaM binding. Furthermore, mutational analyses in the catalytic domain, CnaB-binding helix, and the CaM-binding domains revealed that while the conserved PxIxIT substrate binding motif in CnaA is indispensable for septal localization, CaM is required for its function at the hyphal septum but not for septal localization. We defined an evolutionarily conserved novel mode of calcineurin regulation by phosphorylation in filamentous fungi in a region absent in humans. These findings suggest the possibility of harnessing this unique SPRR for innovative antifungal drug design to combat invasive aspergillosis.
烟曲霉是免疫功能低下患者的主要传染性杀手。钙调神经磷酸酶是一种由钙调蛋白(CaM)依赖性蛋白磷酸酶组成的蛋白,由钙调神经磷酸酶 A(CnaA)和钙调神经磷酸酶 B(CnaB)亚基组成,定位于菌丝尖端和隔膜处,以指导烟曲霉的侵袭和毒力。在这里,我们鉴定了一个位于两个保守的 CnaA 结构域之间的新型丝氨酸-脯氨酸丰富区域(SPRR),该区域位于 CnaB 结合螺旋和 CaM 结合结构域之间,该区域在进化上是保守的,并且是丝状真菌所特有的,而在人类钙调神经磷酸酶中完全不存在。磷酸肽富集和串联质谱分析揭示了体内烟曲霉 CnaA 在 SPRR 中四个聚集的丝氨酸残基(S406、S408、S410 和 S413)处的磷酸化。突变 SPRR 丝氨酸残基以阻止磷酸化导致菌丝生长和毒力缺陷显著,表明钙调神经磷酸酶在 SPRR 处的磷酸化对于其活性和功能是必需的。用来自致病性担子菌新生隐球菌、致病性毛霉 Mucor circinelloides、密切相关的丝状真菌粗糙脉孢菌和植物病原体稻瘟病菌的 cnaA 同源物对烟曲霉ΔcnaA 菌株进行互补分析,揭示了 CnaA 在 SPRR 中的丝状真菌特异性磷酸化和依赖于 SPRR 同源性的菌丝生长恢复。令人惊讶的是,圆二色性研究表明,尽管靠近 CnaA 的 CaM 结合结构域,但在 CaM 结合后,SPRR 的磷酸化不会改变蛋白折叠。此外,在催化结构域、CnaB 结合螺旋和 CaM 结合结构域中的突变分析表明,虽然 CnaA 中的保守 PxIxIT 底物结合基序对于隔膜定位是必不可少的,但 CaM 对于其在菌丝隔膜中的功能是必需的,但不是对于隔膜定位。我们定义了一种在人类中不存在的丝状真菌中钙调神经磷酸酶通过磷酸化调节的进化保守的新型模式。这些发现表明,利用这个独特的 SPRR 进行创新的抗真菌药物设计来对抗侵袭性曲霉菌病是有可能的。