Drug conjugate with multiple targeting ligands having cell endocytosis mediating function

Abstract

The invention discloses a drug conjugate with multiple targeting ligands having a cell endocytosis mediating function. The drug conjugate consists of drug molecules and connexons coupled with the drug molecules; the drug conjugate at least comprises two or more ligands which can be specifically bound to cell surface receptors; the ligands at least include one first ligand which has the cell endocytosis mediating function; and at least one of the ligands and the first ligand are coupled and then are selectively coupled with the drug molecules or the connexons so as to form the drug couplet. The drug conjugate provided by the invention has the beneficial effects that by combining targeting and endocytosis structures, polypeptide, which is targeted by any ligands, is taken as a guiding part, so that the targeting scope of the like medicines is widened. The affinity and the targeting performance of the drug conjugate on diseased cells can be enhanced by virtue of the multiple targeting ligands, so that efficient toxin drugs such as MMAE can be carried, efficacy can be enhanced, a therapeutic window can be widened and side effects of the medicines can be avoided.

Description

technical field [0001] The invention relates to a drug conjugate, in particular to a multi-targeting ligand-drug conjugate with a cell endocytosis mediating function, and belongs to the field of biomedical chemistry. Background technique [0002] Usually, the pathological and physiological characteristics of diseased cells are significantly different from those of normal cells, one of which is the specific or overexpressed substances (such as: antigens, chemical signals, receptors, etc.) on the surface of diseased cells. No expression or low expression. Antibody-drug conjugates (ADCs) and polypeptide-drug conjugates (PDCs) treat diseases based on this principle. Although some drugs have been marketed or entered clinical research, due to the principle of drug design, ADC and PDC drugs have great limitations in clinical application. [0003] ADC is currently mainly used in the field of tumor therapy. The targeting antibody used has a very high affinity for tumor cell surfac...

AI Technical Summary

Problems solved by technology

Therefore, when they are coupled with conventional chemotherapeutic drugs (such as doxorubicin, paclitaxel), the curative effect is low, and after coupling with high-efficiency drug molecules (such as MMAE, DM1, etc.), which are commonly used in ADCs, the toxicity is high, and the effective dose for tumor treatment will lead to animal poisoning death

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