Department of Chronic Disease Epidemiology, Yale School of Public Health, Yale University, New Haven, Connecticut, USA.
Department of Environmental Health Sciences, Yale School of Public Health, Yale University, New Haven, Connecticut, USA.
Int J Cancer. 2025 Jan 1;156(1):52-68. doi: 10.1002/ijc.35104. Epub 2024 Jul 22.
Survival differences exist in colorectal cancer (CRC) patients by sex and disease stage. However, the potential molecular mechanism(s) are not well understood. Here we show that asparagine synthetase (ASNS) and G protein-coupled estrogen receptor-1 (GPER1) are critical sensors of nutrient depletion and linked to poorer outcomes for females with CRC. Using a 3D spheroid model of isogenic SW48 KRAS wild-type (WT) and G12A mutant (MT) cells grown under a restricted nutrient supply, we found that glutamine depletion inhibited cell growth in both cell lines, whereas ASNS and GPER1 expression were upregulated in KRAS MT versus WT. Estradiol decreased growth in KRAS WT but had no effect on MT cells. Selective GPER1 and ASNS inhibitors suppressed cell proliferation with increased caspase-3 activity of MT cells under glutamine depletion condition particularly in the presence of estradiol. In a clinical colon cancer cohort from The Cancer Genome Atlas, both high GPER1 and ASNS expression were associated with poorer overall survival for females only in advanced stage tumors. These results suggest KRAS MT cells have mechanisms in place that respond to decreased nutrient supply, typically observed in advanced tumors, by increasing the expression of ASNS and GPER1 to drive cell growth. Furthermore, KRAS MT cells are resistant to the protective effects of estradiol under nutrient deplete conditions. The findings indicate that GPER1 and ASNS expression, along with the interaction between nutrient supply and KRAS mutations shed additional light on the mechanisms underlying sex differences in metabolism and growth in CRC, and have clinical implications in the precision management of KRAS mutant CRC.
结直肠癌(CRC)患者的生存存在性别和疾病阶段差异。然而,其潜在的分子机制尚不清楚。在这里,我们表明天冬酰胺合成酶(ASNS)和 G 蛋白偶联雌激素受体-1(GPER1)是营养缺乏的关键传感器,与 CRC 女性患者的不良预后相关。我们使用在受限制的营养供应下生长的同源 SW48 KRAS 野生型(WT)和 G12A 突变(MT)细胞的 3D 球体模型发现,谷氨酰胺耗竭抑制了两种细胞系的细胞生长,而 KRAS MT 中 ASNS 和 GPER1 的表达上调。雌二醇降低了 KRAS WT 细胞的生长,但对 MT 细胞没有影响。选择性 GPER1 和 ASNS 抑制剂在谷氨酰胺耗竭条件下抑制 MT 细胞的增殖,并增加 caspase-3 活性,尤其是在存在雌二醇的情况下。在癌症基因组图谱(TCGA)的临床结肠癌队列中,高 GPER1 和 ASNS 表达与女性晚期肿瘤的总生存率较差相关,仅在女性中相关。这些结果表明,KRAS MT 细胞具有应对营养供应减少的机制,通常在晚期肿瘤中观察到,通过增加 ASNS 和 GPER1 的表达来驱动细胞生长。此外,KRAS MT 细胞在营养耗竭条件下对雌二醇的保护作用具有抗性。这些发现表明,GPER1 和 ASNS 表达以及营养供应与 KRAS 突变之间的相互作用进一步揭示了 CRC 中代谢和生长性别差异的潜在机制,并在 KRAS 突变 CRC 的精准管理中具有临床意义。