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Synthesis and evaluation of TLR7/8 and STING agonist conjugates of tumor-targeted cancer immunotherapy

Yi Huang (UGent)
(2024)
Author
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(UGent)
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Abstract
In my doctoral research, I focused on the design and synthesis of tumor-targeted delivery systems for innate immune agonists, particularly TLR7/8 and STING agonists. I developed lipid-conjugated and HMC-conjugated versions of IMDQ and diABZI to enhance their pharmacokinetics and tumor selectivity. These conjugates were formulated into lipid nanoparticles (LNPs) and lipid nanodiscs (LNDs), which significantly improved their accumulation in tumors and activation of innate immune responses. To further enhance tumor specificity, I incorporated MMP-2-sensitive PEGylated constructs (PGGP and PP) onto the particle surface, enabling enzyme-triggered PEG shedding and deeper tumor penetration. This strategy not only reduced off-target toxicity but also boosted immune activation in tumor-draining lymph nodes. My work demonstrated potent anti-tumor efficacy, reshaped the tumor microenvironment, and induced long-term immunological memory, highlighting a promising path for clinical translation of innate immune agonists in cancer immunotherapy.

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Citation

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MLA
Huang, Yi. Synthesis and Evaluation of TLR7/8 and STING Agonist Conjugates of Tumor-Targeted Cancer Immunotherapy. Ghent University. Faculty of Pharmaceutical Sciences, 2024.
APA
Huang, Y. (2024). Synthesis and evaluation of TLR7/8 and STING agonist conjugates of tumor-targeted cancer immunotherapy. Ghent University. Faculty of Pharmaceutical Sciences, Ghent, Belgium.
Chicago author-date
Huang, Yi. 2024. “Synthesis and Evaluation of TLR7/8 and STING Agonist Conjugates of Tumor-Targeted Cancer Immunotherapy.” Ghent, Belgium: Ghent University. Faculty of Pharmaceutical Sciences.
Chicago author-date (all authors)
Huang, Yi. 2024. “Synthesis and Evaluation of TLR7/8 and STING Agonist Conjugates of Tumor-Targeted Cancer Immunotherapy.” Ghent, Belgium: Ghent University. Faculty of Pharmaceutical Sciences.
Vancouver
1.
Huang Y. Synthesis and evaluation of TLR7/8 and STING agonist conjugates of tumor-targeted cancer immunotherapy. [Ghent, Belgium]: Ghent University. Faculty of Pharmaceutical Sciences; 2024.
IEEE
[1]
Y. Huang, “Synthesis and evaluation of TLR7/8 and STING agonist conjugates of tumor-targeted cancer immunotherapy,” Ghent University. Faculty of Pharmaceutical Sciences, Ghent, Belgium, 2024.
@phdthesis{01JRC81Q277NJT4J77ZV82YAFX,
  abstract     = {{In my doctoral research, I focused on the design and synthesis of tumor-targeted delivery systems for innate immune agonists, particularly TLR7/8 and STING agonists. I developed lipid-conjugated and HMC-conjugated versions of IMDQ and diABZI to enhance their pharmacokinetics and tumor selectivity. These conjugates were formulated into lipid nanoparticles (LNPs) and lipid nanodiscs (LNDs), which significantly improved their accumulation in tumors and activation of innate immune responses. To further enhance tumor specificity, I incorporated MMP-2-sensitive PEGylated constructs (PGGP and PP) onto the particle surface, enabling enzyme-triggered PEG shedding and deeper tumor penetration. This strategy not only reduced off-target toxicity but also boosted immune activation in tumor-draining lymph nodes. My work demonstrated potent anti-tumor efficacy, reshaped the tumor microenvironment, and induced long-term immunological memory, highlighting a promising path for clinical translation of innate immune agonists in cancer immunotherapy.}},
  author       = {{Huang, Yi}},
  language     = {{eng}},
  pages        = {{328}},
  publisher    = {{Ghent University. Faculty of Pharmaceutical Sciences}},
  school       = {{Ghent University}},
  title        = {{Synthesis and evaluation of TLR7/8 and STING agonist conjugates of tumor-targeted cancer immunotherapy}},
  year         = {{2024}},
}