クリックケミストリーによるペプチド環化: 効率的かつ正確な環化技術

クリックケミストリーによるペプチド環化: 効率的かつ正確な環化技術

Research background and challenges

Peptide cyclisation is an important strategy to enhance peptide stability, biological activity and selectivity. Traditional cyclisation methods (例えば. 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. しかし, 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

技術的な利点

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.

管理者のアバター

ゼジュン・ペン

最高技術責任者; ペプチド合成のエキスパート コアの専門知識: 複雑なペプチド合成, 非天然アミノ酸修飾, 環状ペプチドとステープルペプチドの構築.

バイオグラフィー:Zejun Peng は有機化学とペプチド合成において豊富な経験を持っています. 彼は固相ペプチド合成の組み合わせ応用に熟達しています。 (SPSS) および液相ペプチド合成 (LPPS), 特に「合成が非常に難しいシーケンス」を克服することに長けています。 (超長鎖ペプチドなど, 疎水性の高い配列, および複数のジスルフィド結合の折り畳み). 彼のリーダーシップの下で, チームはいくつかの特殊な変更で技術的なボトルネックを克服することに成功しました。 (N-メチル化など, PEG化, そして蛍光標識), 以上の合成成功率を維持する 98%.

事実確認済み & 編集ガイドライン
レビュー者: 対象分野の専門家
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