Wang Haiqin, Liang Long, Xie Yifang, Gong Han, Fan Feifan, Wen Chengcai, Jiang Yu, Lei Shiying, Qiu Xili, Peng Hongling, Ye Mao, Xiao Xiaojuan, Liu Jing
Department of Hematology, the Second Xiangya Hospital; School of Life Sciences; Hunan Province Key Laboratory of Basic and Applied Hematology, Central South University, Changsha, Hunan, 410011, China.
Molecular Science and Biomedicine Laboratory (MBL), State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Biology, College of Chemistry and Chemical Engineering, Aptamer Engineering Center of Hunan Province, Hunan University, Changsha, Hunan, 410082, China.
Oncogene. 2025 Mar;44(10):694-708. doi: 10.1038/s41388-024-03245-4. Epub 2024 Dec 9.
Multiple myeloma (MM), the world's second most common hematologic malignancy, poses considerable clinical challenges due to its aggressive progression and resistance to therapy. Addressing these challenges requires a detailed understanding of the mechanisms driving MM initiation, progression, and therapeutic resistance. This study identifies the pseudokinase tribble homolog 3 (TRIB3) as a high-risk factor that promotes MM malignancy in vitro and in vivo. Mechanistically, TRIB3 directly interacts with structure-specific recognition protein 1 (SSRP1) and ubiquitin-specific peptidase 10 (USP10), facilitating the formation of a TRIB3/USP10/SSRP1 ternary complex. This complex stabilizes SSRP1 via USP10-mediated deubiquitination, thereby driving MM cell proliferation. Furthermore, a stapled peptide, SP-A, was developed, which effectively disrupts the TRIB3/USP10/SSRP1 complex, leading to a decrease in SSRP1 levels by inhibiting its stabilization through USP10. Notably, SP-A exhibits strong synergistic effects when combined with the proteasome inhibitor bortezomib. Given the critical role of the TRIB3/USP10/SSRP1 complex in MM pathophysiology, it represents a promising therapeutic target for MM treatment. In MM cells, TRIB3, USP10 and SSRP1 form a ternary complex and TRIB3 enhances the deubiquitinating effect of USP10 on SSRP1, leading to malignant progression of MM. In the case of drug intervention, SP-A attenuates the binding of SSRP1 and USP10 by inhibiting protein interactions between TRIB3 and SSRP1 and promoted SSRP1 protein degradation, leading to significant inhibition of MM development. Visual abstract created with Biorender.
多发性骨髓瘤(MM)是全球第二常见的血液系统恶性肿瘤,因其侵袭性进展和对治疗的耐药性而带来了相当大的临床挑战。应对这些挑战需要详细了解驱动MM起始、进展和治疗耐药的机制。本研究确定假激酶三兄弟同源物3(TRIB3)是促进MM在体外和体内恶性发展的高危因素。从机制上讲,TRIB3直接与结构特异性识别蛋白1(SSRP1)和泛素特异性肽酶10(USP10)相互作用,促进TRIB3/USP10/SSRP1三元复合物的形成。该复合物通过USP10介导的去泛素化作用使SSRP1稳定,从而驱动MM细胞增殖。此外,还开发了一种环肽SP-A,它能有效破坏TRIB3/USP10/SSRP1复合物,通过抑制USP10对SSRP1的稳定作用导致SSRP1水平降低。值得注意的是,SP-A与蛋白酶体抑制剂硼替佐米联合使用时表现出强大的协同作用。鉴于TRIB3/USP10/SSRP1复合物在MM病理生理学中的关键作用,它是MM治疗中一个有前景的治疗靶点。在MM细胞中,TRIB3、USP10和SSRP1形成三元复合物,TRIB3增强USP10对SSRP1的去泛素化作用,导致MM的恶性进展。在药物干预的情况下,SP-A通过抑制TRIB3与SSRP1之间的蛋白质相互作用减弱SSRP1与USP10的结合,并促进SSRP1蛋白降解,从而显著抑制MM的发展。使用Biorender创建的可视化摘要。