Department of Pathology, University of Alabama at Birmingham, Birmingham, Alabama.
Vanderbilt Center for Immunobiology, Vanderbilt University School of Medicine, Nashville, Tennessee.
Cancer Res. 2021 Nov 1;81(21):5425-5437. doi: 10.1158/0008-5472.CAN-20-1723. Epub 2021 Jul 21.
Elevated infiltration of immunosuppressive alternatively polarized (M2) macrophages is associated with poor prognosis in patients with cancer. The tumor microenvironment remarkably orchestrates molecular mechanisms that program these macrophages. Here we identify a novel role for oncogenic Hedgehog (Hh) signaling in programming signature metabolic circuitries that regulate alternative polarization of tumor-associated macrophages. Two immunocompetent orthotopic mouse models of mammary tumors were used to test the effect of inhibiting Hh signaling on tumor-associated macrophages. Treatment with the pharmacologic Hh inhibitor vismodegib induced a significant shift in the profile of tumor-infiltrating macrophages. Mass spectrometry-based metabolomic analysis showed Hh inhibition induced significant alterations in metabolic processes, including metabolic sensing, mitochondrial adaptations, and lipid metabolism. In particular, inhibition of Hh in M2 macrophages reduced flux through the UDP-GlcNAc biosynthesis pathway. Consequently, O-GlcNAc-modification of STAT6 decreased, mitigating the immune-suppressive program of M2 macrophages, and the metabolically demanding M2 macrophages shifted their metabolism and bioenergetics from fatty acid oxidation to glycolysis. M2 macrophages enriched from vismodegib-treated mammary tumors showed characteristically decreased O-GlcNAcylation and altered mitochondrial dynamics. These Hh-inhibited macrophages are reminiscent of inflammatory (M1) macrophages, phenotypically characterized by fragmented mitochondria. This is the first report highlighting the relevance of Hh signaling in controlling a complex metabolic network in immune cells. These data describe a novel immunometabolic function of Hh signaling that can be clinically exploited. SIGNIFICANCE: These findings illustrate that Hh activity regulates a metabolic and bioenergetic regulatory program in tumor-associated macrophages that promotes their immune-suppressive polarization.
免疫抑制性替代极化(M2)巨噬细胞的浸润增加与癌症患者的预后不良有关。肿瘤微环境显著协调了编程这些巨噬细胞的分子机制。在这里,我们发现致癌 Hedgehog(Hh)信号在编程调节肿瘤相关巨噬细胞替代极化的特征代谢回路方面具有新的作用。使用两种免疫活性的同源原位乳腺癌模型来测试抑制 Hh 信号对肿瘤相关巨噬细胞的影响。用药理学 Hh 抑制剂 vismodegib 治疗诱导了肿瘤浸润巨噬细胞特征的显著变化。基于质谱的代谢组学分析显示,Hh 抑制诱导了代谢过程的显著改变,包括代谢感应、线粒体适应和脂质代谢。特别是,在 M2 巨噬细胞中抑制 Hh 会降低 UDP-GlcNAc 生物合成途径的通量。因此,STAT6 的 O-GlcNAc 修饰减少,减轻了 M2 巨噬细胞的免疫抑制程序,而代谢需求较高的 M2 巨噬细胞将其代谢和生物能从脂肪酸氧化转移到糖酵解。从用 vismodegib 治疗的乳腺肿瘤中富集的 M2 巨噬细胞表现出特征性的 O-GlcNAc 修饰减少和线粒体动力学改变。这些受 Hh 抑制的巨噬细胞类似于炎症(M1)巨噬细胞,表型特征为线粒体碎片化。这是首次报道 Hh 信号在控制免疫细胞中复杂代谢网络的相关性。这些数据描述了 Hh 信号的一种新的免疫代谢功能,可以在临床上加以利用。意义:这些发现表明,Hh 活性调节肿瘤相关巨噬细胞中的代谢和生物能调节程序,促进其免疫抑制极化。