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Cell-Based Kinetic Target-Guided Synthesis of an Enzyme Inhibitor
Umeå University, Faculty of Science and Technology, Department of Chemistry.
Umeå University, Faculty of Science and Technology, Department of Chemistry.
2018 (English)In: ACS Medicinal Chemistry Letters, ISSN 1948-5875, E-ISSN 1948-5875, Vol. 9, no 4, p. 351-353Article in journal (Refereed) Published
Abstract [en]

Finding a new drug candidate for a selected target is an expensive and time-consuming process. Target guided-synthesis, or in situ click chemistry, is a concept where the drug target is used to template the formation of its own inhibitors from reactive building blocks. This could simplify the identification of drug candidates. However, with the exception of one example of an RNA-target, target-guided synthesis has always employed purified targets. This limits the number of targets that can be screened by the method. By applying methods from the field of metabolomics, we demonstrate that target-guided synthesis with protein targets also can be performed directly in cell-based systems. These methods offer new possibilities to conduct screening for drug candidates of difficult protein targets in cellular environments.

Place, publisher, year, edition, pages
2018. Vol. 9, no 4, p. 351-353
Keyword [en]
target-guided synthesis, in situ click chemistry, enzyme catalysis, drug discovery
National Category
Medicinal Chemistry
Identifiers
URN: urn:nbn:se:umu:diva-147832DOI: 10.1021/acsmedchemlett.7b00535ISI: 000430256200010PubMedID: 29670699OAI: oai:DiVA.org:umu-147832DiVA, id: diva2:1207104
Available from: 2018-05-18 Created: 2018-05-18 Last updated: 2018-06-09Bibliographically approved

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Antti, HenrikSellstedt, Magnus

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