Kou Songzi, Sun Chenbo, Chen Weitao, Gao Hanyu, Sun Fei
Greater Bay Biomedical Innocenter, Shenzhen Bay Laboratory, Shenzhen, China.
Shenzhen Key Laboratory for Neuronal Structural Biology, Biomedical Research Institute, Shenzhen Peking University-The Hong Kong University of Science and Technology Medical Center, Shenzhen, China.
Angew Chem Int Ed Engl. 2025 Aug 18;64(34):e202509419. doi: 10.1002/anie.202509419. Epub 2025 Jun 25.
Mirror-image proteins and nucleic acids exhibit remarkable biostability and bioorthogonality, offering a promising strategy to enhance the longevity of biological therapeutics. Here, we present a modular approach for constructing complex protein architectures that integrate both natural-chirality (L-) and mirror-image (D-) motifs. Key to this strategy is the development of D-SpyStapler-a chemically synthesized, chirally inverted ligase that enables the efficient conjugation of D-SpyTag and D-BDTag. By exploiting the achirality of glycine (Gly), we used L-sortase to covalently link D-peptides (e.g., SpyTag or BDTag, bearing an N-terminal poly-Gly motif) to L-proteins (e.g., GFP, VLP-forming Mi3, or antigens) containing a C-terminal LPXTG sorting signal. The resulting D-SpyTagged and D-BDTagged proteins were further assembled via D-SpyStapler. This method enabled the construction of chirally chimeric VLP vaccines displaying antigens derived from malaria parasites and coronaviruses in various forms-recombinant proteins or synthetic peptides-providing significant flexibility and modularity for vaccine design. The resulting chirally hybrid vaccines exhibited enhanced proteolytic resistance in vitro and elicited potent immune responses in vivo. This study provides a versatile platform for developing long-acting therapeutics and vaccines.
镜像蛋白质和核酸具有显著的生物稳定性和生物正交性,为提高生物治疗药物的寿命提供了一种有前景的策略。在此,我们提出了一种构建复杂蛋白质结构的模块化方法,该方法整合了天然手性(L-)和镜像(D-)基序。该策略的关键是开发D-SpyStapler——一种化学合成的、手性反转的连接酶,它能够实现D-SpyTag和D-BDTag的高效共轭。通过利用甘氨酸(Gly)的非手性,我们使用L-分选酶将D-肽(例如,带有N端多甘氨酸基序的SpyTag或BDTag)与含有C端LPXTG分选信号的L-蛋白质(例如,GFP、形成VLP的Mi3或抗原)共价连接。所得的D-SpyTagged和D-BDTagged蛋白质通过D-SpyStapler进一步组装。该方法能够构建以各种形式(重组蛋白或合成肽)展示源自疟原虫和冠状病毒的抗原的手性嵌合VLP疫苗,为疫苗设计提供了显著的灵活性和模块化。所得的手性杂交疫苗在体外表现出增强的抗蛋白水解能力,并在体内引发了强烈的免疫反应。这项研究为开发长效治疗药物和疫苗提供了一个通用平台。