13095-73-3Relevant articles and documents
A self-assembled, ROS-responsive Janus-prodrug for targeted therapy of inflammatory bowel disease
Li, Shanshan,Xie, Aiqing,Li, Hui,Zou, Xiang,Zhang, Qixiong
, p. 66 - 78 (2019)
A self-assembled and oxidation-degradable Janus-prodrug, termed as Bud-ATK-Tem (B-ATK-T), was fabricated by ROS-responsive aromatized thioketal (ATK) linked anti-inflammatory drug budesonide (Bud) and antioxidant tempol (Tem). Benefiting from the hydrophobic interactions and π-π stacking interactions of ATK, prodrug B-ATK-T could self-assemble into nanoparticles (NP) in water containing lecithin and DSPE-PEG2K. The morphology of B-ATK-T NP (approximate 100–120 nm) was confirmed to be regular spherical by transmission electron microscope. B-ATK-T NP was endowed high drug loading content with 41.23% for Bud and 15.55% for Tem. The rapid drug release from B-ATK-T NP proceeded in an extensive reactive oxygen species (ROS)-dependent manner. More than 98% of Bud and Tem in B-ATK-T NP could release in the mimic inflammation microenvironment or phorbol-12-myristate-13-acetate (PMA)-stimulated macrophages within short time. The release of drugs in a simultaneous and proportional manner ensures that B-ATK-T NP can increase the combined efficacy of anti-inflammation and anti-oxidation. It is worth noting that B-ATK-T NP could be passively accumulated and dramatically increasing the maximum drugs concentration in the inflamed colon of mice with inflammatory bowel disease (IBD) by oral route, and avoiding potential systemic side effects. B-ATK-T NP could not only relieve colitis via inhibiting the expression of oxidative and proinflammatory mediators more than combination of free drugs, but also significantly reduce colitis-caused death. Taken together, the self-assembled, Janus-prodrug B-ATK-T NP is a promising candidate therapies for IBD, even for other inflammatory diseases.
Her2 targeted polypeptide drug conjugate as well as a preparation method and application thereof
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Paragraph 0048; 0058-0060, (2020/05/30)
The invention relates to an Her2 targeted polypeptide drug conjugate as well as a preparation method and application thereof. The Her2 targeted polypeptide drug conjugate has a molecular structural formula shown in a formula I, wherein Aaa1 is L or D type Lys or Arg; Aaa2 is L or D type Lys or Arg; X is CH2, NH or O; ROH is a hydrophobic antitumor drug; and n is 1 or 2. The Her2 targeted polypeptide drug conjugate provided by the invention can realize targeted drug delivery, the targeted polypeptide can transport the antitumor drug to specific tumor cells, the drug enters the tumor cells and then exerts the characteristic of specific degradation of disulfide bonds at tumor sites, and the antitumor drug is rapidly released. Compared with conventional joint arms such as 2,2'-dithiodiglycolicacid and 3,3'-dithiodipropionic acid, the Her2 targeted polypeptide drug conjugate provided by the invention has the advantages that an anticancer drug in the form of an original drug molecule can beobtained without further hydrolysis, the drug efficacy is improved, and the toxic and side effects on normal cells are reduced.
Based on molecular glue of the fluorescence-labeled nucleotide and its use in DNA sequencing
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Paragraph 0102; 0104, (2018/01/05)
The invention discloses a fluorescence labelled nucleotide based on a molecular glue and a use thereof in DNA sequencing. The structure formula of the fluorescence labelled nucleotide is shown in a formula (I) in the specification, wherein R1 is shown in the specification, R2 is fluorescein or shown in the specification, and dNTP is ribonucleoside triphosphote which contains four different base groups; the fluorescein is selected from one of the BODIPY, rhodamine, coumarin, xanthene, cyanin, pyrene, phthalocyanine, alexa, a squarene dye, a composition for generating energy transfer dye and the derivatives thereof. The fluorescence labelled nucleotide can be used for DNA sequencing; simultaneously the raw materials for synthesizing the fluorescence labelled nucleotide are simple and easy to obtain and the fluorescence labelled nucleotide can be used for large-scale popularization. The biological assessment result shows that all the requirements of the high-throughput sequencing biochemical reaction can be satisfied by the reversible terminal, and the reversible terminal has good practical prospect.
