Kawai-Kawachi Asuka, Lenormand Madison M, Astier Clémence, Herbel Noé, Cutrona Meritxell B, Ngo Carine, Garrido Marlène, Eychenne Thomas, Dorvault Nicolas, Bordelet Laetitia, Song Feifei, Bouyakoub Ryme, Loktev Anastasia, Romo-Morales Antonio, Henon Clémence, Colmet-Daage Léo, Vibert Julien, Drac Marjorie, Brough Rachel, Schwob Etienne, Martella Oliviano, Pinna Guillaume, Shipley Janet M, Mittnacht Sibylle, Zimmermann Astrid, Gulati Aditi, Mir Olivier, Le Cesne Axel, Faron Matthieu, Honoré Charles, Lord Christopher J, Chabanon Roman M, Postel-Vinay Sophie
The ATIP-Avenir Inserm and ERC StG (Epi)genetic Vulnerabilities in Solid Tumors and Sarcoma Laboratory, Inserm Unit UMR 981, Université Paris-Saclay, Gustave Roussy, Villejuif, France.
Cancer RNA Research Unit, National Cancer Center Research Institute, Tokyo, Japan.
Cancer Res. 2025 Jan 2;85(1):154-170. doi: 10.1158/0008-5472.CAN-23-3603.
Desmoplastic small round cell tumor (DSRCT) is an aggressive sarcoma subtype that is driven by the EWS-WT1 chimeric transcription factor. The prognosis for DSRCT is poor, and major advances in treating DSRCT have not occurred for over two decades. To identify effective therapeutic approaches to target DSRCT, we conducted a high-throughput drug sensitivity screen in a DSRCT cell line assessing chemosensitivity profiles for 79 small-molecule inhibitors. DSRCT cells were sensitive to PARP inhibitors (PARPi) and ataxia-telangiectasia and Rad3-related inhibitors (ATRi), as monotherapies and in combination. These effects were recapitulated using multiple clinical PARPi and ATRi in three biologically distinct, clinically relevant models of DSRCT, including cell lines, a patient-derived xenograft-derived organoid model, and a cell line-derived xenograft mouse model. Mechanistically, exposure to a combination of PARPi and ATRi caused increased DNA damage, G2-M checkpoint activation, micronuclei accumulation, replication stress, and R-loop formation. EWS-WT1 silencing abrogated these phenotypes and was epistatic with exogenous expression of the R-loop resolution enzyme RNase H1 in reversing sensitivity to PARPi and ATRi monotherapies. The combination of PARPi and ATRi also induced EWS-WT1-dependent cell-autonomous activation of the cyclic GMP-AMP synthase-stimulator of IFN genes innate immune pathway and cell-surface expression of PD-L1. Taken together, these findings point toward a role for EWS-WT1 in generating R-loop-dependent replication stress that leads to a targetable vulnerability, providing a rationale for the clinical assessment of PARPi and ATRi in DSRCT. Significance: EWS-WT1, the unique oncogenic driver of desmoplastic small round cell tumors, confers sensitivity to PARP and ATR inhibitors, supporting the potential of these drugs in treating patients with this aggressive sarcoma subtype.
促纤维增生性小圆细胞肿瘤(DSRCT)是一种侵袭性肉瘤亚型,由EWS-WT1嵌合转录因子驱动。DSRCT的预后很差,二十多年来在DSRCT治疗方面没有取得重大进展。为了确定针对DSRCT的有效治疗方法,我们在一种DSRCT细胞系中进行了高通量药物敏感性筛选,评估了79种小分子抑制剂的化学敏感性谱。DSRCT细胞对聚(ADP-核糖)聚合酶抑制剂(PARPi)和共济失调毛细血管扩张症及Rad3相关抑制剂(ATRi)敏感,无论是作为单一疗法还是联合使用。在三种生物学上不同的、临床相关的DSRCT模型中,包括细胞系、患者来源的异种移植衍生类器官模型和细胞系衍生的异种移植小鼠模型,使用多种临床PARPi和ATRi再现了这些效果。从机制上讲,暴露于PARPi和ATRi的组合会导致DNA损伤增加、G2-M检查点激活、微核积累、复制应激和R环形成。EWS-WT1沉默消除了这些表型,并且在逆转对PARPi和ATRi单一疗法的敏感性方面,与R环解决酶核糖核酸酶H1的外源性表达呈上位关系。PARPi和ATRi的组合还诱导了EWS-WT1依赖性的环鸟苷酸-腺苷酸合成酶-干扰素基因刺激物先天免疫途径的细胞自主激活以及程序性死亡受体1(PD-L1)的细胞表面表达。综上所述,这些发现表明EWS-WT1在产生R环依赖性复制应激中起作用,这种应激导致了一个可靶向的脆弱性,为PARPi和ATRi在DSRCT中的临床评估提供了理论依据。意义:EWS-WT1是促纤维增生性小圆细胞肿瘤独特的致癌驱动因素,赋予对PARP和ATR抑制剂的敏感性,支持这些药物治疗这种侵袭性肉瘤亚型患者的潜力。