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Polypeptide-drug conjugate with tumor directed therapy effect, and its application

A technology of therapeutic effect and conjugate, applied in the field of biomedicine, can solve the problems of reducing normal tissue damage and high drug loading

Active Publication Date: 2014-12-31
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, the drug-loading capacity of the polypeptide-drug conjugate is relatively high, which reduces its damage to normal tissues

Method used

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  • Polypeptide-drug conjugate with tumor directed therapy effect, and its application
  • Polypeptide-drug conjugate with tumor directed therapy effect, and its application
  • Polypeptide-drug conjugate with tumor directed therapy effect, and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0089] The synthesis of embodiment 1 compound 2

[0090] 2-Aminoethanol (1.2g, 20mmol) and 5N NaOH solution (4.8mL) were dissolved in dioxane / H 2 In a mixed solvent of O (15mL / 7mL), Boc 2 O (5.0g, 23mmol) was dissolved in dioxane, the diluted Boc 2 O was slowly added dropwise to the reaction system, stirred overnight at room temperature, concentrated, extracted with 10% citric acid solution and ethyl acetate, and the organic phase was washed with anhydrous Na 2 SO 4 After drying, the solvent was spin-dried to obtain pure compound 2 (2.7 g, 85%).

Embodiment 2

[0091] The synthesis of embodiment 2 compound 3

[0092] The obtained compound 2 (1.6g, 10mmol), N-hydroxysuccinimide (1.79g, 11mmol) and triphenylphosphine (2.88g, 11mmol) were dissolved in 25mL DCM, and at 0°C, DEAD (1.92g, 11mmol) was added to the reaction system, stirred overnight at room temperature, the solvent was spin-dried and passed through the column to obtain pure product 3 (2.91g, 95%).

Embodiment 3

[0093] The synthesis of embodiment 3 compound 4

[0094] The obtained compound 3 (1.78g, 5.8mmol) was dissolved in 10mL of ethanol, and then hydrazine hydrate (187L, 5.97mmoL) was slowly added dropwise to the reaction system, a white precipitate appeared in the system, and the reaction was monitored by TLC until the substrate After consumption, it was filtered, the filtrate was concentrated, and passed through a column to obtain pure compound 4 (800mg, 78%).

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Abstract

The invention relates to a polypeptide-drug conjugate with a tumor directed therapy effect, and a preparation method and an application thereof. The polypeptide-drug conjugate can specifically convey PD0325901 analog to cancer cells over-expressing integrin alphavbeta3 in order to realize the directed therapy effect of tumors.

Description

technical field [0001] The invention relates to a polypeptide-drug conjugate with tumor-guiding therapeutic effect and application thereof. The invention belongs to the technical field of biomedicine. Background technique [0002] The signal transduction pathway is an important way for the cells of the body to transmit information and transport substances with the outside world, and is an important life activity for the survival of cells. Tumor cells use the excessive activation of various signaling pathways to accelerate tumor cell proliferation, differentiation, invasion, migration, and inhibit cell apoptosis, leading to the occurrence and development of cancer. Including the PI3K / mTOR / AKT pathway, JAK / STAT pathway and MAPK pathway, various signal transduction pathways are more or less involved in the development of tumors, and are currently hot molecular targets for anti-tumor drug research. The ERK signal transduction pathway is in a pivotal position in the cell signal...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/166A61P35/00
Inventor 武芸陈自立候建军李肖肖
Owner PEKING UNIV
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