At 17:49 Beijing time on October 4th, the Swedish Academy of Sciences announced the award of the 2022 Nobel Prize in Chemistry to Carolyn R. Bertozzi, Morten Meldal and K. Barry Sharpless for their contributions to the fields of click chemistry and biological orthogonal chemistry.
A synthesis concept initially proposed by Sharpless in 1998 and gradually perfected thereafter——Click chemistry. The core idea is: Synthetic chemistry should be guided by molecular functions, and through the simple splicing of small units, the chemical synthesis of various molecules can be completed quickly and reliably.
The theory is beautiful, but the reality is cruel. The selectivity of many reactions is not high, and the reaction rate is too slow to conform to the concept of click chemistry. with the support of their theory, Shapleis and Meldal completed what is regarded as the crown jewel of click chemistry, the copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction. This is a simple and effective chemical reaction, but without (I) copper, there will be numerous side reactions, once the addition of (I) copper, the reaction is rapid and the product is single. The reaction is now being used to develop drugs, map DNA molecules and create more suitable materials.
From this, it is not difficult to see that the most difficult thing in the construction of molecules is to find suitable catalyst atoms, and atoms of transition elements have become bright pearls in click chemistry.
Imagine that if people find enough click reactions, as long as there are some molecules with simple structures, the corresponding substances can be quickly synthesized, then the future pharmaceutical and material preparation will greatly save energy and time, and be more environmentally friendly and green.
Bertozzi proposed the concept of bioorthogonal chemistry in 2003, which refers to those chemical reactions that can be carried out in living cells or tissues without interfering with the biochemical reactions of the organism itself. It is like building a laboratory in living cells, and these reactions must conform to the characteristics of click chemistry in order to be carried out precisely in cells.
The research of bioorthogonal chemistry can accurately locate target cells and target drugs in cancer treatment. Through this bioorthogonal fluorescence method, new ideas can be proposed for the treatment of cancer patients. It can also be used to explore cell structure, biomolecular interaction mechanisms in organs, decipher disease processes, and help drug development.
“For the classic click chemistry and related reactions, we can provide various PEG derivatives and click chemistry reagents to assist customers’ scientific research and drug research and development” said the R&D director of Biopharma PEG, “We supply polyethylene glycol products and reagents with azide, alkyne, DBCO and other cyclooctane for for Copper-Free Click Chemistry.”
Click chemistry and non-copper bioorthogonal reactions have made important progress in the field of biomedical research. Click chemistry enables specific labeling of cellular target proteins and can be used to adhere cells together, as well as enable efficient and effective molecular imaging and drug delivery for diagnostic and therapeutic purposes. Click chemistry can also be used to develop molecular tools, such as DNA nanocatalysts, chemical synthesis of genomic DNA, assisted CRISPR-Cas gene editing, ADC and PROTAC synthesis, etc. Overall, click chemistry has become a valuable tool in the biomedical field and in organic chemistry.
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