The DOI matches its Crossref record; 76 of the 76 references it cites were found in a registry or an index.
In situ click chemistry: probing the binding landscapes of biological molecules
Abstract
Combinatorial approaches to the discovery of new functional molecules are well established among chemists and biologists, inspired in large measure by the modular composition of many systems and molecules in Nature. Many approaches rely on the synthesis and testing of individual members of a candidate combinatorial library, but attention has also been paid to techniques that allow the target to self-assemble its own binding agents. These fragment-based methods, grouped under the general heading of target-guided synthesis (TGS), show great promise in lead discovery applications. In this tutorial review, we review the use of the 1,3-dipolar cycloaddition reaction of organic azides and alkynes in a kinetically-controlled TGS approach, termed in situ click chemistry. The azide-alkyne reaction has several distinct advantages, most notably high chemoselectivity, very low background ligation rates, facile synthetic accessibility, and the stability and properties of the 1,2,3-triazole products. Examples of the discovery of potent inhibitors of acetylcholinesterases, carbonic anhydrase, HIV-protease, and chitinase are described, as are methods for the templated assembly of agents that bind DNA and proteins.
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Cites
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The growing applications of click chemistry
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Dynamic Combinatorial Chemistry
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Copper-free click chemistry for dynamic in vivo imaging
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Cited by
In situ click chemistry generation of cyclooxygenase-2 inhibitors
Bhardwaj, A., Kaur, J., Wuest, M., & Wuest, F. (2017) · Nature Communications · doi:10.1038/s41467-016-0009-6 · Cited by 7,448
Modulators of Protein–Protein Interactions
Milroy, L.-G., Grossmann, T. N., Hennig, S., Brunsveld, L., & Ottmann, C. (2014) · Chemical Reviews · doi:10.1021/cr400698c · Cited by 497
Chemoproteomics and Chemical Probes for Target Discovery
Drewes, G., & Knapp, S. (2018) · Trends in Biotechnology · doi:10.1016/j.tibtech.2018.06.008 · Cited by 132
Metadata
- Authors
- Mamidyala, S. K., & Finn, M. G.
- Venue
- Chemical Society Reviews
- Publisher
- Royal Society of Chemistry (RSC)
- Published
- 2010
- Volume
- 39
- Issue
- 4
- Pages
- 1252
- ISSN
- 0306-0012 (ISSN-L)
- 1460-4744
- OpenAlex
- W1971170829
- Cited by
- 489
- References
- 76
- FWCI
- 1.88
- Type
- journal article
- Language
- en
- Open access
- closed
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