The 2022 Nobel Prize in Chemistry Goes to Carolyn R. Bertozzi, Morten Meldal, and K. Barry Sharpless - ACS Axial | ACS Publications
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The 2022 Nobel Prize in Chemistry Goes to Carolyn R. Bertozzi, Morten Meldal, and K. Barry Sharpless

The Nobel Prize in Chemistry 2022 was awarded to Carolyn R. Bertozzi, Morten Meldal, and K. Barry Sharpless “for the development of click chemistry and bioorthogonal chemistry,” which involve simple, quick chemical reactions that can occur within living organisms without disrupting normal biological functions.

“We are absolutely delighted with these awards, which recognize the enormous impact of click chemistry and bioorthogonal chemistry,” says ACS President Angela K. Wilson. “This type of chemistry links together chemical building blocks in a predictable way, almost like Lego®. Putting these building blocks together opens up a range of possibilities from drug development to materials to diagnostics.”

Bertozzi has a long-standing history with ACS. She has been a member for 32 years and is an ACS Fellow. She is also the founding and current Editor-in-Chief of ACS Central Science, the first fully open-access journal from ACS Publications. She has won numerous awards; notably, the Roger Adams Award in Organic Chemistry for 2023; the Arthur C. Cope Award in 2017; the ACS Award in Pure Chemistry in 2001; and an Arthur C. Cope Scholar Award in 1999. She has published more than 150 articles ACS journals and provided thought-provoking commentary in many editorials, a collection of which we have shared below.

Meldal has been a member of ACS for 14 years. In 2009, he received the Ralph F. Hirschmann Award in Peptide Chemistry. Meldal has published over 40 articles in ACS journals.

Sharpless is no stranger to the Nobel Prize in Chemistry. He received the award in 2001 for his work on chirally catalyzed oxidation reactions. An ACS Fellow, Sharpless has been a member of the Society for 59 years and has published almost 150 articles in ACS journals. He also coined the term “click chemistry” at the 217th ACS National Meeting in 1999 in his abstract, “Click Chemistry: A Concept for Merging Process and Discovery Chemistry.” He has received many awards, including the Priestley Medal (sponsored by ACS) in 2019; the Roger Adams Award in Organic Chemistry in 1997; the Arthur C. Cope Award in 1992; an Arthur C. Cope Scholar Award in 1986; and the ACS Award for Creative Work in Synthetic Organic Chemistry, in 1983.

All three winners have each published extensively in ACS Publications journals throughout the years. The following articles from each of the laureates, as well as a collection of additional papers associated with the winning research, will be made free-to-read for the remainder of 2022 in honor of their win.

Carolyn R. Bertozzi

A Strain-Promoted [3 + 2] Azide−alkyne Cycloaddition for Covalent Modification of Biomolecules in Living Systems
J. Am. Chem. Soc. 2004, 126, 46, 15046–15047
DOI: 10.1021/ja044996f

Aminooxy-, Hydrazide-, and Thiosemicarbazide-Functionalized Saccharides: Versatile Reagents for Glycoconjugate Synthesis
J. Org. Chem. 1998, 63, 21, 7134–7135
DOI: 10.1021/jo981351n

A “Traceless” Staudinger Ligation for the Chemoselective Synthesis of Amide Bonds
Org. Lett. 2000, 2, 14, 2141–2143
DOI: 10.1021/ol006054v

A Fluorogenic Dye Activated by the Staudinger Ligation
J. Am. Chem. Soc. 2003, 125, 16, 4708–4709
DOI: 10.1021/ja029013y

Chemoselective Approaches to Glycoprotein Assembly
Acc. Chem. Res. 2001, 34, 9, 727–736
DOI: 10.1021/ar9901570

Rapid Cu-Free Click Chemistry with Readily Synthesized Biarylazacyclooctynones
J. Am. Chem. Soc. 2010, 132, 11, 3688–3690
DOI: 10.1021/ja100014q

Second-Generation Difluorinated Cyclooctynes for Copper-Free Click Chemistry
J. Am. Chem. Soc. 2008, 130, 34, 11486–11493
DOI: 10.1021/ja803086r

A Comparative Study of Bioorthogonal Reactions with Azides
ACS Chem. Biol. 2006, 1, 10, 644–648
DOI: 10.1021/cb6003228

Morten Meldal

Peptidotriazoles on Solid Phase:  [1,2,3]-Triazoles by Regiospecific Copper(I)-Catalyzed 1,3-Dipolar Cycloadditions of Terminal Alkynes to Azides
J. Org. Chem. 2002, 67, 9, 3057–3064
DOI: 10.1021/jo011148j

K. Barry Sharpless

Copper(I)-Catalyzed Synthesis of Azoles. DFT Study Predicts Unprecedented Reactivity and Intermediates
J. Am. Chem. Soc. 2005, 127, 1, 210–216
DOI: 10.1021/ja0471525 

Related ACS Publications Articles

Influence of strain on chemical reactivity. Relative reactivity of torsionally strained double bonds in 1,3-dipolar cycloadditions
Shea, K. J. and Kim, J. S. J. Am. Chem. Soc. 1992, 114, 12, 4846–4855
DOI: 10.1021/ja00038a059

Heats of hydrogenation. IX. Cyclic acetylenes and some miscellaneous olefins
Turner, R. B. et al. J. Am. Chem. Soc. 1973, 95, 3, 790–792.
DOI: 10.1021/ja00784a025

Staudinger Ligation: A Peptide from a Thioester and Azide
Nilsson, B. L. et al. Org. Lett. 2000, 2, 13, 1939–1941
DOI: 10.1021/ol0060174

A new amino protecting group removable by reduction. Chemistry of the dithiasuccinoyl (Dts) function
Barany, G. and Merrifield, R. B. J. Am. Chem. Soc. 1977, 99, 22, 7363–7365
DOI: 10.1021/ja00464a050

Tetrazine Ligation: Fast Bioconjugation Based on Inverse-Electron-Demand Diels−Alder Reactivity
Blackman, M. et al. J. Am. Chem. Soc. 2008, 130, 41, 13518–13519
DOI: 10.1021/ja8053805

Tetrazine-Based Cycloadditions: Application to Pretargeted Live Cell Imaging
Devaraj, N. K. et al. Bioconjugate Chem. 2008, 19, 12, 2297–2299
DOI: 10.1021/bc8004446

Learn More About the 2022 Nobel Prize in Chemistry winners in C&EN.

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Further Reading

Articles: Carolyn R. Bertozzi

From Mechanism to Mouse: A Tale of Two Bioorthogonal Reactions
Acc. Chem. Res. 2011, 44, 9, 666–676
DOI: 10.1021/ar200148z

Cell Surface Engineering by a Modified Staudinger Reaction
https://www.science.org/doi/full/10.1126/science.287.5460.2007

Copper-free click chemistry for dynamic in vivo imaging
https://www.pnas.org/doi/abs/10.1073/pnas.0707090104

Engineering Chemical Reactivity on Cell Surfaces Through Oligosaccharide Biosynthesis
https://www.science.org/doi/full/10.1126/science.276.5315.1125

Copper-Free Click Chemistry in Living Animals
https://www.pnas.org/doi/abs/10.1073/pnas.0911116107

In Vivo Imaging of Membrane-Associated Glycans in Developing Zebrafish
https://www.science.org/doi/full/10.1126/science.1155106

Articles: Morten Meldal

Peptidotriazoles: Copper(I)-Catalyzed 1,3-Dipolar Cycloadditions on Solid-Phase
Peptides: The Wave of the Future. American Peptide Symposia, vol 7. Springer, Dordrecht.
DOI: 10.1007/978-94-010-0464-0_119

Computational Evolution of Threonine-Rich β-Hairpin Peptides Mimicking Specificity and Affinity of Antibodies
ACS Cent. Sci. 2019, 5, 2, 259–269
DOI: 10.1021/acscentsci.8b00614

Cu-Catalyzed Azide−Alkyne Cycloaddition
Chem. Rev. 2008, 108, 8, 2952–3015
DOI: 10.1021/cr0783479

Articles: K. Barry Sharpless

Sulfur [18F]Fluoride Exchange Click Chemistry Enabled Ultrafast LateStage Radiosynthesis
J. Am. Chem. Soc. 2021, 143, 10, 3753–3763
DOI: 10.1021/jacs.0c09306

Sulfur(VI) Fluoride Exchange (SuFEx)-Enabled High-Throughput Medicinal Chemistry
J. Am. Chem. Soc. 2020, 142, 25, 10899–10904
DOI: 10.1021/jacs.9b13652

SuFEx Click Chemistry Enabled Late-Stage Drug Functionalization
J. Am. Chem. Soc. 2018, 140, 8, 2919–2925
DOI: 10.1021/jacs.7b12788

In Situ Click Chemistry:  Enzyme Inhibitors Made to Their Own Specifications
J. Am. Chem. Soc. 2004, 126, 40, 12809–12818
DOI: 10.1021/ja046382g

Editorials: Carolyn R. Bertozzi

The Centrality of Chemistry (Inaugural ACS Central Science editorial)
ACS Cent. Sci. 2015, 1, 1, 1–2
DOI: 10.1021/acscentsci.5b00090

Achieving Gender Balance in the Chemistry Professoriate Is Not Rocket Science
ACS Cent. Sci. 2016, 2, 4, 181–182
DOI: 10.1021/acscentsci.6b00102

Ingredients for a Positive Safety Culture
ACS Cent. Sci. 2016, 2, 11, 764–766
DOI: 10.1021/acscentsci.6b00341

Postdoc Labor Love
ACS Cent. Sci. 2016, 2, 6, 359–360
DOI: 10.1021/acscentsci.6b00167

A Decade of Bioorthogonal Chemistry
Acc. Chem. Res. 2011, 44, 9, 651–653
DOI: 10.1021/ar200193f

Related Special Issues

Bioorthogonal Chemistry in Biology Special Issue

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