Contact

  • Academic
    pengwei@stanford.edu
    University - Student Department: Rad/Radiological Sciences Laboratory Position: Graduate

Additional Info

  • Mail Code: 5488

All Publications

  • Radiotherapy activates picolinium prodrugs in tumours. Nature chemistry Fu, Q., Gu, Z., Shen, S., Bai, Y., Wang, X., Xu, M., Sun, P., Chen, J., Li, D., Liu, Z. 2024

    Abstract

    Radiotherapy-induced prodrug activation provides an ideal solution to reduce the systemic toxicity of chemotherapy in cancer therapy, but the scope of the radiation-activated protecting groups is limited. Here we present that the well-established photoinduced electron transfer chemistry may pave the way for developing versatile radiation-removable protecting groups. Using a functional reporter assay, N-alkyl-4-picolinium (NAP) was identified as a caging group that efficiently responds to radiation by releasing a client molecule. When evaluated in a competition experiment, the NAP moiety is more efficient than other radiation-removable protecting groups discovered so far. Leveraging this property, we developed a NAP-derived carbamate linker that releases fluorophores and toxins on radiation, which we incorporated into antibody-drug conjugates (ADCs). These designed ADCs were active in living cells and tumour-bearing mice, highlighting the potential to use such a radiation-removable protecting group for the development of next-generation ADCs with improved stability and therapeutic effects.

    View details for DOI 10.1038/s41557-024-01501-4

    View details for PubMedID 38561425

    View details for PubMedCentralID 6470858

  • Bioorthogonal chemistry for prodrug activation in vivo CHEMICAL SOCIETY REVIEWS Fu, Q., Shen, S., Sun, P., Gu, Z., Bai, Y., Wang, X., Liu, Z. 2023: 7737-7772

    Abstract

    Prodrugs have emerged as a major strategy for addressing clinical challenges by improving drug pharmacokinetics, reducing toxicity, and enhancing treatment efficacy. The emergence of new bioorthogonal chemistry has greatly facilitated the development of prodrug strategies, enabling their activation through chemical and physical stimuli. This "on-demand" activation using bioorthogonal chemistry has revolutionized the research and development of prodrugs. Consequently, prodrug activation has garnered significant attention and emerged as an exciting field of translational research. This review summarizes the latest advancements in prodrug activation by utilizing bioorthogonal chemistry and mainly focuses on the activation of small-molecule prodrugs and antibody-drug conjugates. In addition, this review also discusses the opportunities and challenges of translating these advancements into clinical practice.

    View details for DOI 10.1039/d2cs00889k

    View details for Web of Science ID 001098310200001

    View details for PubMedID 37905601