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Click Chemistry: Novel Applications in Cell Biology and Drug Discovery

Dr. Matthias Gehringer

Eberhard Karls Universität Tübingen, Institute of Pharmaceutical Sciences, Pharmaceutical and Medicinal Chemistry, Auf der Morgenstelle 8, 72076 Tübingen, Germany

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Prof. Dr. Stefan A. Laufer,

Corresponding Author

Prof. Dr. Stefan A. Laufer

[email protected]

Eberhard Karls Universität Tübingen, Institute of Pharmaceutical Sciences, Pharmaceutical and Medicinal Chemistry, Auf der Morgenstelle 8, 72076 Tübingen, Germany

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Dr. Matthias Gehringer,

Dr. Matthias Gehringer

Eberhard Karls Universität Tübingen, Institute of Pharmaceutical Sciences, Pharmaceutical and Medicinal Chemistry, Auf der Morgenstelle 8, 72076 Tübingen, Germany

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Prof. Dr. Stefan A. Laufer,

Corresponding Author

Prof. Dr. Stefan A. Laufer

[email protected]

Eberhard Karls Universität Tübingen, Institute of Pharmaceutical Sciences, Pharmaceutical and Medicinal Chemistry, Auf der Morgenstelle 8, 72076 Tübingen, Germany

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First published: 25 October 2017

https://doi.org/10.1002/anie.201710195

Citations: 28

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Graphical Abstract

A safe BET: Apart from target engagement, subcellular location and tissue distribution are critical parameters in drug discovery. A novel, generalizable approach has been reported that involves exploiting click chemistry to elucidate these parameters. By using clickable analogues of known Bromodomain and extraterminal domain (BET) inhibitors, various labels were introduced in situ and utilized to determine the biological fate of these probes.

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Volume56, Issue49

December 4, 2017

Pages 15504-15505

Click Chemistry: Novel Applications in Cell Biology and Drug Discovery

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