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In Situ Click Chemistry: Enzyme Inhibitors Made to Their Own Specifications
Abstract
The in situ click chemistry approach to lead discovery employs the biological target itself for assembling inhibitors from complementary building block reagents via irreversible connection chemistry. The present publication discusses the optimization of this target-guided strategy using acetylcholinesterase (AChE) as a test system. The application of liquid chromatography with mass spectroscopic detection in the selected ion mode for product identification greatly enhanced the sensitivity and reliability of this method. It enabled the testing of multicomponent mixtures, which may dramatically increase the in situ screening throughput. In addition to the previously reported in situ product syn-TZ2PA6, we discovered three new inhibitors, syn-TZ2PA5, syn-TA2PZ6, and syn-TA2PZ5, derived from tacrine and phenylphenanthridinium azides and acetylenes, in the reactions with Electrophorus electricus and mouse AChE. All in situ-generated compounds were extremely potent AChE inhibitors, because of the presence of multiple sites of interaction, which include the newly formed triazole nexus as a significant pharmacophore.
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Tornøe, C. W., Christensen, C., & Meldal, M. (2002) · The Journal of Organic Chemistry · doi:10.1021/jo011148j · Cited by 8,696
Drug research: myths, hype and reality
Kubinyi, H. (2003) · Nature Reviews Drug Discovery · doi:10.1038/nrd1156 · Cited by 348
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
The growing applications of click chemistry
Moses, J. E., & Moorhouse, A. D. (2007) · Chem. Soc. Rev. · doi:10.1039/b613014n · Cited by 2,367
Ladmiral, V., Mantovani, G., Clarkson, G. J., Cauet, S., Irwin, J. L., & Haddleton, D. M. (2006) · Journal of the American Chemical Society · doi:10.1021/ja058364k · Cited by 586
Lossouarn, A., Renard, P.-Y., & Sabot, C. (2021) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.0c00568 · Cited by 26
SIGLEC-4 (MAG) antagonists: From the natural carbohydrate epitope to glycomimetics
Schwardt, O., Kelm, S., & Ernst, B. (2013) · Topics in current chemistry · doi:10.1007/128_2013_498 · Cited by 14
Metadata
- Authors
- Manetsch, R., Krasiński, A., Radić, Z., Raushel, J., Taylor, P., Sharpless, K. B., & Kolb, H. C.
- Venue
- Journal of the American Chemical Society
- Publisher
- American Chemical Society (ACS)
- Published
- 2004-09-18
- Volume
- 126
- Issue
- 40
- Pages
- 12809-12818
- ISSN
- 0002-7863 (ISSN-L)
- 1520-5126
- OpenAlex
- W2008742048
- Cited by
- 423
- References
- 2
- FWCI
- 18.22
- Type
- journal article
- Language
- en
- Open access
- closed
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- Manetsch, R., Krasiński, A., Radić, Z., Raushel, J., Taylor, P., Sharpless, K. B., & Kolb, H. C. (2004). In Situ Click Chemistry: Enzyme Inhibitors Made to Their Own Specifications. Journal of the American Chemical Society. https://doi.org/10.1021/ja046382g
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