Chemija pagrįsta peptidų ciklizacija: efektyvi ir tiksli ciklizacijos technologija

Chemija pagrįsta peptidų ciklizacija: efektyvi ir tiksli ciklizacijos technologija

Research background and challenges

Peptide cyclisation is an important strategy to enhance peptide stability, biological activity and selectivity. Traditional cyclisation methods (e.g. chemical cross-linking, enzymatic cyclisation) suffer from low efficiency and many side reactions. Click chemistry, as an efficient and modular synthetic method, provides a new solution for peptide cyclisation. Tačiau, the traditional click chemistry method has poor selectivity, can only react at a single site, and has harsh reaction conditions, which limits its application in the field of peptide cyclisation. Based on click chemistry, we rely on the introduction of a modular design, and have successfully combined click chemistry with peptide cyclisation to achieve highly efficient and precise cyclisation technology.


Technological breakthrough

Innovative peptide cyclisation design: We have developed new peptide cyclisation methods based on click chemistry reactions such as CuAAC, SPAAC, and inverse electron demand Diels-Alder reaction.
Pioneering modular design: achieving rapid referencing of different moieties for peptide functionalization

Technical Advantages

High efficiency and precision: effectively improve the cyclisation efficiency, high selectivity, low by-products and simple purification.
Mild reaction conditions: no need for violent reaction conditions, applicable to a variety of easily degradable peptides.
Modular design: easy to introduce different functional groups to achieve peptide functionalization.

Areas of application

Click chemistry-driven peptide cyclisation technology has a wide range of application prospects in the following fields:
Peptide drug research and development: improve the stability, biological activity and cell membrane permeability of peptide drugs, and develop new peptide drugs.
Biomaterials: construct functionalized peptide materials for tissue engineering, drug delivery and other fields.
Chemical biology: study peptide-protein interactions and develop novel biological probes and drug targets.


Click chemistry-driven peptide cyclisation is a highly efficient and precise cyclisation technique, which provides new tools and methods for peptide cyclisation and has a broad application prospect. With the continuous development of click chemistry technology, it is believed that this technology will play an increasingly important role in the field of peptide science.

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Zejunas Pengas

vyriausiasis technologijų pareigūnas; Peptidų sintezės ekspertas Pagrindinė kompetencija: Sudėtinga peptidų sintezė, nenatūralios aminorūgščių modifikacijos, ir ciklinių peptidų bei susegtų peptidų konstravimas.

Biografija:Zejun Peng turi didelę organinės chemijos ir peptidų sintezės patirtį. Jis išmano kombinuotą kietosios fazės peptidų sintezės taikymą (SPSS) ir skystosios fazės peptidų sintezė (LPPS), ir yra ypač įgudęs įveikti „labai sunkiai sintezuojamas sekas“ (pvz., itin ilgos grandinės peptidai, labai hidrofobinės sekos, ir daugybinis disulfidinis ryšys). Jam vadovaujant, komanda sėkmingai įveikė technines kliūtis keliose specializuotose modifikacijose (pavyzdžiui, N-metilinimas, PEGilinimas, ir fluorescencinis ženklinimas), išlaikant sintezės sėkmės rodiklį 98%.

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