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Acc Chem Res. 2007 Oct;40(10):1025-33. Epub 2007 Jun 5.

Tagged small molecule library approach for facilitated chemical genetics.

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  • 1Department of Chemistry, New York University, New York, New York 10003, USA.


Chemical genetics is a powerful method which utilizes small molecule regulators to reveal the molecular basis of diverse biological processes. However, the current chemical genetic approach sometimes meets a serious bottleneck during the process of target identification. One faces difficulty in conjugating the active compound to an affinity matrix without losing or reducing its activity that leads to laborious structure-activity relationship (SAR) studies. To facilitate this process, we have developed a tagged triazine library containing a built-in linker that provides a straightforward transition from phenotypic screening to target identification. A strategy for constructing a tagged library and applications with a streamlined target identification and subsequent mechanistic study are discussed in this Account.

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