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Liu J, Si S, Xu J, et al. Construction of synergistic pH/H. Bioorg Chem. 2021;119:105510doi: 10.1016/j.bioorg.2021.105510.
Liu, J., Si, S., Xu, J., Xue, P., & Li, K. (2021). Construction of synergistic pH/H. Bioorganic chemistry, 119105510. https://doi.org/10.1016/j.bioorg.2021.105510
Liu, Jun, et al. "Construction of synergistic pH/H." Bioorganic chemistry vol. 119 (2021): 105510. doi: https://doi.org/10.1016/j.bioorg.2021.105510
Liu J, Si S, Xu J, Xue P, Li K. Construction of synergistic pH/H. Bioorg Chem. 2021 Nov 23;119:105510. doi: 10.1016/j.bioorg.2021.105510. Epub 2021 Nov 23. PMID: 34847429.
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Bioorg Chem. 2021 Nov 23;119:105510. doi: 10.1016/j.bioorg.2021.105510. Epub 2021 Nov 23.

Construction of synergistic pH/H.

Bioorganic chemistry

Jun Liu, Shuang Si, Jinyi Xu, Peng Xue, Kaipeng Li

Affiliations

  1. College of Chemistry and Chemical Engineering, Hexi University, Zhangye City 734000, Gansu Province, PR China. Electronic address: [email protected].
  2. College of Chemistry and Chemical Engineering, Hexi University, Zhangye City 734000, Gansu Province, PR China.

PMID: 34847429 DOI: 10.1016/j.bioorg.2021.105510

Abstract

We have developed a real-time and multifunctional doxifluridine-conjugate prodrug (LYX), which involved the preliminary methylfluorescein with 5-fluorouracil linker as protecting group, the targeting biotin unit, and a model therapeutic drug (doxifluridine). The shielding group (5'-DFUR) was found to be effective in prolonging circulation at physiological pH 7.4 and improving accumulation in the acidic microenvironment of the tumor. Based on this strategy, the stability and stimulus responsive properties of prodrug could enhance drug release efficiency and exhibit fewer side effects, thereby providing a unique opportunity for diagnosis and imaging additional analytes or enzymatic activities.

Copyright © 2021 Elsevier Inc. All rights reserved.

Keywords: Blood circulation; Cellular internalization; Prodrug; pH/H(2)O(2)

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