Biotinylation, the functional addition of a biotin molecule to a biologically active compound (small molecules) represents a common technique for identification of the intracellular binding partners that underlie the foundation of observed biological activity of the molecule. Many advances in the area of small molecule biotinylation have come about in recent years due to the explosion of advances in the fields of bioorthogonal chemistry and proteomics. Deciphering the mode of action and biological protein target of a drug candidate provides vital information on off-target effects, potential interactions, and other data valuable for bringing the compound to the clinic. However, the identification of such biological targets is extremely difficult in the area of chemical biology. One of the ways to overcome this problem is the use of biotinylated compounds for the identification of the target proteins. In this poster we describe the methods for attaching the biotin moiety to some of our preclinical (ON 24160, ON 24860 and ON 1231360) and clinical (ON 01910, ON 03105 and ON 01210) compounds and we show the target identification using some of these biotinylated compounds.

Biotinylation of small molecules for target identification

247th National Meeting (2014)

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