Li Fanni, Wang Jingmei, Liu Tianya, Yang Wenguang, Li Yong, Sun Qi, Yan Jin, He Wangxiao
Department of Medical Oncology and Department of Talent Highland, The First Affiliated Hospital of Xi'an Jiaotong University, Xi'an, 710061, P. R. China.
Institute for Stem Cell & Regenerative Medicine, The Second Affiliated Hospital of Xi'an Jiaotong University, Xi'an, 710004, China.
Small. 2024 Dec;20(52):e2404892. doi: 10.1002/smll.202404892. Epub 2024 Oct 21.
Despite the availability of immune checkpoint inhibitors (ICBs) significantly prolonging the life expectancy of some lung adenocarcinoma (LUAD) patients, their implementation and long-term effectiveness are hampered by the growing issue of acquired resistance. Herein, the bioinformatics analysis of immunotherapy-resistant LUAD patients and the system analysis of Anti-PD1-resistant mice models once again validate that the resistance-associated Wnt/β-catenin pathway offers a promising avenue for ICB sensitization. Consequently, a mild and convenient self-assembly between albumin and carnosic acid (CA), a Wnt inhibitor is employed, to develop a supramolecular albumin known as ABCA, serving as a reactivator for ICB. As anticipated, ABCA effectively suppress the Wnt/β-catenin cascade in vitro and leads to significant inhibition of cell proliferation while promoting apoptosis. Most notably, ABCA restores the anticancer efficacy of Anti-PD1 in immunotherapy-resistant LUAD orthotopic allografting mice models by reinvigorating the adaptive immune response mediated by T lymphocytes. Furthermore, ABCA exhibits minimal adverse effects during treatment and high-dose toxicity tests, underscoring its excellent potential for clinical translation. Collectively, the present work possesses the potential to provide innovative perspectives on the advancement of optimized immunotherapies targeting drug resistance, while also presenting a promising avenue for translating Wnt inhibitors into immunotherapeutic drugs for their clinical application.
尽管免疫检查点抑制剂(ICB)的应用显著延长了一些肺腺癌(LUAD)患者的预期寿命,但其应用和长期疗效却受到获得性耐药问题日益严重的阻碍。在此,对免疫治疗耐药的LUAD患者进行生物信息学分析,并对抗PD1耐药小鼠模型进行系统分析,再次证实与耐药相关的Wnt/β-连环蛋白通路为ICB致敏提供了一条有前景的途径。因此,利用白蛋白与Wnt抑制剂肌醇六磷酸(CA)之间温和便捷的自组装,开发了一种名为ABCA的超分子白蛋白,作为ICB的再激活剂。正如预期的那样,ABCA在体外有效抑制Wnt/β-连环蛋白级联反应,导致细胞增殖受到显著抑制,同时促进细胞凋亡。最值得注意的是,ABCA通过恢复T淋巴细胞介导的适应性免疫反应,在免疫治疗耐药的LUAD原位同种异体移植小鼠模型中恢复了抗PD1的抗癌疗效。此外,ABCA在治疗和高剂量毒性试验中表现出最小的不良反应,突出了其在临床转化方面的优异潜力。总的来说,目前的工作有可能为优化针对耐药性的免疫疗法提供创新视角,同时也为将Wnt抑制剂转化为免疫治疗药物以供临床应用提供了一条有前景的途径。