Xue Yinyin, Wang Yue, Ren Zhiqiang, Yu Ker
Department of Pharmacology, Fudan University School of Pharmacy, Shanghai, China.
Oncogene. 2025 Mar;44(11):739-752. doi: 10.1038/s41388-024-03248-1. Epub 2024 Dec 10.
Pancreatic ductal adenocarcinoma (PDAC) remains the most challenging human malignancy that urgently needs effective therapy. Tissue factor (TF) is expressed in ~80% of PDAC and represents a potential therapeutic target. While a novel TF-ADC (MRG004A) demonstrated efficacy for PDAC and TNBC in a Phase I/II trial [Ref. 18], the functional role of TF in PDAC remains incompletely understood. We investigated the relationship between TF and the innate STING pathway. We found that patients with TF-overexpression had poor survival, very low levels of P-STING/P-TBK1, reduced amounts of ISGs and chemokines as well as low numbers of cytotoxic immunocytes in their tumor. In experimental models of mouse and human PDAC, tumor cell-intrinsic TF expression played a major role in silencing the cytosolic micronuclei sensing and cGAS-STING activation. This process involved a TREX1 exonuclease-dependent clearance of micronucleus-DNA accumulated in tumor cells. Treatment of tumors with TF-KO/shRNA or anti-TF antibody HuSC1-39 (parent antibody of MRG004A) triggered a rapid and proteasome-dependent degradation of TREX1 thereby restoring the STING/TBK1 cascade phosphorylation. TF-inhibition therapy promoted a robust STING/IRF3-dependent IFN/CCL5/CXCL9-11 production, immune effector cell infiltration and antitumor efficacy. Moreover, in the PBMC and cancer cell co-culture, TF-inhibition synergized with a STING agonist compound. A covalently conjugated TF antibody-STING agonist ADC strongly increased the efficacy of tumor-targeted STING agonism on chemokine secretion and tumor inhibition in vitro and in vivo. Thus, TF-inhibition reshapes an "immune hot" tumor environment. TF-targeted therapy warrants clinical investigation as a single agent or in combination with immunotherapy for treating TF-positive PDAC and TNBC.
胰腺导管腺癌(PDAC)仍然是最具挑战性的人类恶性肿瘤,迫切需要有效的治疗方法。组织因子(TF)在约80%的PDAC中表达,是一个潜在的治疗靶点。虽然一种新型TF-ADC(MRG004A)在一项I/II期试验中对PDAC和三阴性乳腺癌(TNBC)显示出疗效[参考文献18],但TF在PDAC中的功能作用仍未完全明确。我们研究了TF与先天性STING通路之间的关系。我们发现,TF过表达的患者生存率低,肿瘤中P-STING/P-TBK1水平极低,干扰素刺激基因(ISG)和趋化因子数量减少,细胞毒性免疫细胞数量也少。在小鼠和人类PDAC的实验模型中,肿瘤细胞内源性TF表达在沉默胞质微核感应和cGAS-STING激活中起主要作用。这一过程涉及TREX1核酸外切酶依赖性清除肿瘤细胞中积累的微核DNA。用TF基因敲除/短发夹RNA(shRNA)或抗TF抗体HuSC1-39(MRG004A的亲本抗体)治疗肿瘤会引发TREX1的快速且蛋白酶体依赖性降解,从而恢复STING/TBK1级联磷酸化。TF抑制疗法促进了强大的STING/IRF3依赖性干扰素/CCL5/CXCL9-11产生、免疫效应细胞浸润和抗肿瘤疗效。此外,在外周血单核细胞(PBMC)与癌细胞共培养中,TF抑制与一种STING激动剂化合物协同作用。一种共价偶联的TF抗体-STING激动剂ADC在体外和体内均显著增强了肿瘤靶向性STING激动对趋化因子分泌和肿瘤抑制的疗效。因此,TF抑制重塑了一个“免疫热”肿瘤环境。TF靶向治疗作为单一药物或与免疫疗法联合用于治疗TF阳性的PDAC和TNBC值得进行临床研究。