Click Chemistry[1] describes pairs of functional groups that rapidly and selectively react (“click”) with each other under mild, aqueous conditions. The concept of Click Chemistry has been transformed into convenient, versatile and reliable two-step coupling procedures of two molecules A and B[1-5] that are widely used in biosciences[6-8], drug discovery[9] and material science[10].

Click Chemistry background information

 


Click Reagents by Chemistry

Alkyne ReagentsAzide ReagentsDBCO Reagents (DBCO = Dibenzocyclooctyne)Tetrazine ReagentsTCO Reagents (TCO = Transcyclooctene)


Click Reagents by Application

... on DNA ...on RNA ... on Proteins ... in Posttranslational Modification Analysis

 
Advantages of Click Chemistry:

  • Highly selective, low background labeling:
    CLICK-functional groups are inert to naturally occurring functional groups ("bioorthogonal") such as amines
  • Rapid and quantitative labeling
  • Allows non-radioactive analysis of enzymatic activities both in vitro and in vivo: Small-sized CLICK functional groups possess excellent substrate properties


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Selected references:

Introduction to the concept of Click Chemistry

[1] Kolb et al. (2001) Click chemistry: diverse chemical function from a few good reactions. Angew. Chem. Int. Ed. 40 (11):2004.
[2] Sletten et al. (2009) Bioorthogonal Chemistry: Fishing for Selectivity in a Sea of Functionality. Angew. Chem. Int. Ed.48:6998.
[3] Jewett et al.(2010) Cu-free click cycloaddition reactions in chemical biology. Chem. Soc. Rev. 39(4):1272.
[4] Best et al. (2009) Click Chemistry and Bioorthogonal Reactions: Unprecedented Selectivity in the Labeling of Biological Molecules. Biochemistry.48:6571.
[5] Lallana et al. (2011) Reliable and Efficient Procedures for the Conjugation of Biomolecules through Huisgen Azide–Alkyne Cycloadditions. Angew. Chem. Int. Ed. 50:8794.

Overview of Click Chemistry Applications

[6] Grammel et al. (2013) Chemical Reporters for biological discovery. Nature Chemical Biology 9:475.
[7] Xie et al. (2013) Cell-selective metabolic labeling of biomolecules with bioorthogonal functionalities. Current Opinion in Chemical Biology 17:747.
[8] Su et al. (2013) Target identification of biologically active small molecules via in situ methods. Current Opinion in Chemical Biology 17:768.
[9] Zeng et al. (2013) The Growing Impact of Bioorthogonal Click Chemistry on the Development of Radiopharmaceuticals. J Nucl Med 54:829.
[10] Evans et al. (2007) The Rise of Azide–Alkyne 1,3-Dipolar 'Click' Cycloaddition and its Application to Polymer Science and Surface Modification. Australian Journal of Chemistry 60(6):384.