Conjugate of polyethylene glycol monomethyl ether coupled E-selectin peptide ligand and anti-tumor drug and application thereof

A technology of polyethylene glycol monomethyl ether and anti-tumor drugs, which is applied in the field of conjugates of polyethylene glycol monomethyl ether coupled with E-selectin peptide ligands and anti-tumor drugs, can solve problems such as deficiencies, and achieve Easy yield, inhibition of adhesion, good stability

Pending Publication Date: 2019-08-16
TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The most important issue is that most technologies only achieve passive targeting of tumor sites through the EPR effect of nanoparticles, but the drug enrichment efficiency of tumor sites produced by this passive targeting is still relatively low. Further greatly improve the tumor targeting and enrichment of drugs? The phenomenon of tumor spread and migration is very serious. If the tumor can be effectively controlled at the primary site and the tumor cells can be further killed, this is a very efficient treatment method, but the current research on this aspect is still very lacking

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  • Conjugate of polyethylene glycol monomethyl ether coupled E-selectin peptide ligand and anti-tumor drug and application thereof
  • Conjugate of polyethylene glycol monomethyl ether coupled E-selectin peptide ligand and anti-tumor drug and application thereof
  • Conjugate of polyethylene glycol monomethyl ether coupled E-selectin peptide ligand and anti-tumor drug and application thereof

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Embodiment Construction

[0062] The embodiments of the present invention will be described in detail below. It should be noted that the embodiments are illustrative, not restrictive, and cannot limit the protection scope of the present invention.

[0063] The raw materials used in the present invention, unless otherwise specified, are conventional commercially available products; the methods used in the present invention, unless otherwise specified, are conventional methods in the art.

[0064] A conjugate of polyethylene glycol monomethyl ether coupling E-selectin peptide ligand and antitumor drug, the conjugate is composed of E-selectin peptide ligand, polyethylene glycol monomethyl ether, hydrophobic anti-tumor Preparation of tumor drugs;

[0065] Wherein, the E-selectin peptide ligands are IELLQAR, IDLMQAR, DITWDQLWDLMK, DITWDELWKIMN, RNMSWLELWEHMK, DLWDWVVGKPAG sequence polypeptides and reverse sequence peptides, cyclic peptides, and D-configuration polypeptides of these polypeptides; the polyeth...

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Abstract

The invention relates to a conjugate of polyethylene glycol monomethyl ether coupled E-selectin peptide ligand and an anti-tumor drug. The conjugate is prepared from an E-selectin peptide ligand, polyethylene glycol monomethyl ether, and a hydrophobic anti-tumor drug. The conjugate takes a water-soluble mPEG as a carrier, which allows the conjugate to self-assemble into nanoparticles in an aqueoussolution, and passively targets the tumor site by the EPR effect. The amphiphilic structure involved in the present invention is easy to form nanomicelles, which has better dispersibility and betterstability than that of the micelles formed by the conjugate with simultaneous modification at both ends.

Description

technical field [0001] The invention belongs to the technical field of new compound synthesis and drug application, in particular to a conjugate of polyethylene glycol monomethyl ether coupling E-selectin peptide ligand and antitumor drug and its application. Background technique [0002] E-selectin is a kind of protein highly expressed in tumor vascular endothelium, which can specifically recognize the terminal domains of certain glycoproteins and glycolipid molecules on the surface of tumor cells. The interaction between tumor cells can make tumor cells adhere to endothelial cells, and then migrate with blood flow, resulting in the diffusion and migration of tumor cells. Therefore, the specific ligand of E-selectin can be used as a targeting molecule to bring other antitumor drugs to the tumor site, and its ligand can also inhibit the migration of tumor cells. Therefore, the design and synthesis of E-selectin ligand and Conjugates of antitumor drugs are expected to achiev...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/60A61K47/64A61K47/69A61K45/00A61K31/4745A61P35/00
CPCA61K47/60A61K47/64A61K47/6907A61K45/00A61K31/4745A61P35/00
Inventor 郭娜郁彭杨尧郝甜甜付颖汤晶晶滕玉鸥
Owner TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
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