Construction of synergistic pH/H2O2-responsive prodrug for prolonging blood circulation and accelerating cellular internalization

Autor:	Jun Liu, Kaipeng Li, Jinyi Xu, Shuang Si, Peng Xue
Rok vydání:	2022
Předmět:	Drug media_common.quotation_subject Organic Chemistry Doxifluridine Prodrug Biochemistry chemistry.chemical_compound Biotin chemistry Blood circulation Drug Discovery Biophysics Internalization Protecting group Molecular Biology Linker media_common
Zdroj:	Bioorganic Chemistry. 119:105510
ISSN:	0045-2068
DOI:	10.1016/j.bioorg.2021.105510
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::f9520e4cad18ee717f0e1533f042bd72 https://doi.org/10.1016/j.bioorg.2021.105510 Zobrazit plný text záznamu Full Text from ScienceDirect