Haidar Malak, Lombès Anne, Bouillaud Frédéric, Kennedy Eileen J, Langsley Gordon
Inserm U1016, CNRS UMR8104, Cochin Institute , Paris 75014 France.
Laboratoire de Biologie Cellulaire Comparative des Apicomplexes, Faculté de Médecine, Université Paris Descartes - Sorbonne Paris Cité , Paris 75014, France.
ACS Infect Dis. 2017 Mar 10;3(3):216-224. doi: 10.1021/acsinfecdis.6b00180. Epub 2017 Jan 24.
Theileria annulata infects bovine leukocytes, transforming them into invasive, cancer-like cells that cause the widespread disease called tropical theileriosis. We report that in Theileria-transformed leukocytes hexokinase-2 (HK2) binds to B cell lymphoma-2-associated death promoter (BAD) only when serine (S) 155 in BAD is phosphorylated. We show that HK2 recruitment to BAD is abolished by a cell-penetrating peptide that acts as a nonphosphorylatable BAD substrate that inhibits endogenous S155 phosphorylation, leading to complex dissociation and ubiquitination and degradation of HK2 by the proteasome. As HK2 is a critical enzyme involved in Warburg glycolysis, its loss forces Theileria-transformed macrophages to switch back to HK1-dependent oxidative glycolysis that down-regulates macrophage proliferation only when they are growing on glucose. When growing on galactose, degradation of HK2 has no effect on Theileria-infected leukocyte proliferation, because metabolism of this sugar is independent of hexokinases. Thus, targeted disruption of the phosphorylation-dependent HK2/BAD complex may represent a novel approach to control Theileria-transformed leukocyte proliferation.
环形泰勒虫感染牛白细胞,将其转化为具有侵袭性的、类似癌细胞的细胞,引发名为热带泰勒虫病的广泛疾病。我们报告称,在泰勒虫转化的白细胞中,己糖激酶-2(HK2)仅在BAD中的丝氨酸(S)155磷酸化时才与B细胞淋巴瘤-2相关死亡促进因子(BAD)结合。我们表明,一种细胞穿透肽可消除HK2与BAD的结合,该肽作为一种不可磷酸化的BAD底物,抑制内源性S155磷酸化,导致复合物解离以及HK2被蛋白酶体泛素化和降解。由于HK2是参与瓦伯格糖酵解的关键酶,其缺失迫使泰勒虫转化的巨噬细胞切换回依赖HK1的氧化糖酵解,而这种糖酵解仅在巨噬细胞以葡萄糖为生长底物时下调巨噬细胞增殖。当以半乳糖为生长底物时,HK2的降解对泰勒虫感染的白细胞增殖没有影响,因为这种糖的代谢不依赖己糖激酶。因此,靶向破坏磷酸化依赖性HK2/BAD复合物可能代表一种控制泰勒虫转化白细胞增殖的新方法。