Polypeptide nano hybrid as well as preparation method and application thereof

Abstract

The invention discloses a polypeptide nano hybrid as well as a preparation method and an application thereof; the general formula of the hybrid is [Au-S-S-peptide]n; the preparation method of the hybrid comprises the following steps: selecting a cysteine-modified polypeptide antagonist, copolymerizing sulfydryl-containing polypeptide and Au ions through domino reaction to generate an Au-polypeptide precursor, and then adding a prefabricated ultra-small gold core, further performing surface reduction through a reduction environment of the solution, and obtaining the polypeptide nano hybrid after reaction equilibrium is achieved. The hybrid is used for inhibiting the growth of tumors; according to the polypeptide nano hybrid obtained by the invention, the interaction of intracellular proteins in tumor cellsand proteinscan be regulated by inhibiting or destroying the mutual combination between beta-catenin and Bcl9, and finally the growth of tumors is inhibited; and the polypeptide nano hybrid prepared by the preparation method disclosed by the invention has the advantages of excellent solution stability and large drug loading capacity.

Description

technical field [0001] The invention belongs to the field of bioengineering, and in particular relates to a polypeptide nano-hybrid and its preparation method and application. Background technique [0002] Intracellular protein-protein interactions (PPIs) play critical roles in all biological systems and are often dysregulated in disease, representing an important but underexploited class of therapeutic targets. Human physiology is estimated to involve more than 400,000 intracellular protein-protein interactions (PPIs), which provide numerous opportunities for pharmacological interventions targeting a variety of diseases. However, the vast majority of PPIs are not inhibited by small molecules, mainly due to the ubiquitous interface of PPIs (~800-2000 A2) in contrast to the deep grooves (~300-500 A2) with affinity small molecules Flat and large. Fortunately, with the advent of peptide therapeutics comes hope: Peptides can mimic the topology of proteins very well, thanks to ...

AI Technical Summary

Problems solved by technology

[0003] However, in practical peptide therapeutics, especially those targeting intracellular PPIs, there are always two inherent deficiencies: poor proteolytic stability and low cell membrane permeability

Although some successes have been achieved in peptide structure-based nanoengineering, great challenges remain in the clinical application of peptide nanoformulations, especially in regulating intracellular protein-protein interactions (PPIs)

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