Koh Mun Yee, Chung Tae-Hoon, Tang Nicole Xin Ning, Toh Sabrina Hui Min, Zhou Jianbiao, Tan Tze King, Chen Leilei, Chng Wee Joo, Teoh Phaik Ju
Cancer Science Institute of Singapore, National University of Singapore, Singapore, Singapore.
Department of Anatomy, Yong Loo Lin School of Medicine, National University of Singapore, Singapore, Singapore.
Blood. 2025 Mar 13;145(11):1164-1181. doi: 10.1182/blood.2024024429.
Immunomodulatory drugs (IMiDs) are a major class of drugs for treating multiple myeloma (MM); however, acquired resistance to IMiDs remains a significant clinical challenge. Although alterations in cereblon and its pathway are known to contribute to IMiD resistance, they account for only 20% to 30% of cases, and the underlying mechanisms in the majority of the resistance cases remain unclear. Here, we identified adenosine deaminase acting on RNA1 (ADAR1) as a novel driver of lenalidomide resistance in MM. We showed that lenalidomide activates the MDA5-mediated double-stranded RNA (dsRNA)-sensing pathway in MM cells, leading to interferon (IFN)-mediated apoptosis, with ADAR1 as the key regulator. Mechanistically, ADAR1 loss increased lenalidomide sensitivity through endogenous dsRNA accumulation, which in turn triggered dsRNA-sensing pathways and enhanced IFN responses. Conversely, ADAR1 overexpression reduced lenalidomide sensitivity, attributed to increased RNA editing frequency, reduced dsRNA accumulation, and suppression of the dsRNA-sensing pathways. In summary, we report the involvement of ADAR1-regulated dsRNA sensing in modulating lenalidomide sensitivity in MM. These findings highlight a novel RNA-related mechanism underlying lenalidomide resistance and underscore the potential of targeting ADAR1 as a novel therapeutic strategy.
免疫调节药物(IMiDs)是治疗多发性骨髓瘤(MM)的一大类药物;然而,对IMiDs产生获得性耐药仍然是一个重大的临床挑战。虽然已知cereblon及其信号通路的改变会导致IMiD耐药,但它们仅占病例的20%至30%,大多数耐药病例的潜在机制仍不清楚。在此,我们确定了作用于RNA1的腺苷脱氨酶(ADAR1)是MM中来那度胺耐药的一个新驱动因素。我们发现来那度胺激活了MM细胞中MDA5介导的双链RNA(dsRNA)感应通路,导致干扰素(IFN)介导的细胞凋亡,其中ADAR1是关键调节因子。从机制上讲,ADAR1缺失通过内源性dsRNA积累增加了来那度胺敏感性,这反过来又触发了dsRNA感应通路并增强了IFN反应。相反,ADAR1过表达降低了来那度胺敏感性,这归因于RNA编辑频率增加、dsRNA积累减少以及dsRNA感应通路的抑制。总之,我们报道了ADAR1调节的dsRNA感应参与调节MM中来那度胺的敏感性。这些发现突出了来那度胺耐药背后一种新的与RNA相关的机制,并强调了靶向ADAR1作为一种新治疗策略的潜力。