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Peptide click chemistry:Precision conjugation for advanced biotech applications

Oct 18, 2025

What is click chemistry?

Click chemistry refers to a class of highly efficient,modular,and reliable chemical reactions that allow rapid assembly of small molecular building blocks.introduced by prof.k.barry sharpless,this concept emphasizes reactions that are fast,selective,high-yielding,and compatible with aqueous or biological environments.

In peptide science,click chemistry has become a powerful tool for peptide ligation,cyclization,bioconjugation,fluorescent labeling,and nanoparticle surface modification.it enables precise,stable,and bioorthogonal linking of peptides with diverse molecules for biomedical applications.

Core click reactions in peptide chemistry

1.cuaac(copper(i)-catalyzed azide–alkyne cycloaddition)

The most widely used click reaction in peptide chemistry.

Involves coupling of an azide(-n₃)and an alkyne(-c≡c-)group to form a 1,2,3-triazole ring under cu(i)catalysis.

The resulting triazole is chemically stable,hydrolysis-resistant,and mimics an amide bond.

2.copper-free click chemistry(spaac)

Avoids cu toxicity in biological systems.

Uses strained alkynes such as dbco or bcn for spontaneous reaction with azides.

Ideal for in vivo labeling,protein conjugation,and live-cell imaging.

3.on-resin or side-chain click reactions

Clickable amino acids can be introduced during spps(solid-phase peptide synthesis).

Enables intramolecular cyclization,peptide elongation,or attachment to dyes,peg,or nanocarriers.

Advantages of click chemistry for peptides

Advantage

Description

High yield&efficiency

Reactions are nearly quantitative with minimal by-products.

Bioorthogonality

Compatible with aqueous and physiological conditions.

Stability

Triazole linkage is robust and mimics natural amide bonds.

Versatility

Connects peptides to polymers,drugs,fluorophores,and biomaterials.

Ease of purification

By-product-free and easy to separate via hplc.


Applications of click chemistry in peptide research

Peptide ligation and extension–linking short peptides to create longer chains.

Peptide cyclization–forming cyclic or stapled peptides to enhance stability and bioactivity.

Peptide–drug or fluorophore conjugation–for targeted delivery and imaging.

Pegylation and nanoparticle functionalization–enhancing solubility and biostability.

Radiolabeling and isotope tagging–precise attachment of imaging agents.

Biorunstar's capabilities in click chemistry peptides

At biorunstar,we provide comprehensive peptide click chemistry services tailored to research and industrial applications:

Custom synthesis of azide-,alkyne-,dbco-,or bcn-functionalized peptides

Cuaac and copper-free spaac conjugation routes

Site-specific click reactions for cyclization,pegylation,and labeling

Peptide-to-nanoparticle or polymer coupling for nanomedicine applications

Purity≥95%(hplc);full qc documentation(ms,coa,and nmr available)We maintain an extensive library of clickable amino acids and linkers,enabling fast turnaround and scalable synthesis from milligram to gram scale.

Related Peptide Products:

DBCO Peptide Synthesis Case

Semaglutide (Lys20(N₃-CH₂CO-))

Mazdutide (Lys20(N₃-CH₂CO-))

Tirzepatide (Lys20(N₃-CH₂CO-))

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