Small-molecule target identification techniques

XAV939 Affinity Tool Bead Surrogate Affinity Matrix Inactive Control  

The use of affinity probes for in-lysate quantitative affinity chemical proteomics is discussed in Section 3.6, and illustrated with the XAV939 linker-bearing analog. 

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Small-molecule target identification techniques are a hypothesis generating endeavor, requiring follow-up experimental verification. Once the potential targets are identified, the effort has just begun and the modulation of the protein must be corroborated - or ruled out - by methods orthogonal to the one used... 

Table 4.2 Summary chart of small-molecule target identification techniques [44].

This book offers you the contemporary knowledge and techniques necessary to understand the entire research field of chemical biology. New technologies to dissect the interactions between small molecules and proteins are introduced with some examples of the identification of binding proteins of small molecules. The final chapter will be useful to get a bird s-eye view of recent progress on small molecules targeting proteins. 

Chemistry plays a key role in the discovery of novel therapeutic targets to address unmet medical needs. In this chapter, we have reviewed its use and impact in the context of phenotypic screening where, in connection to cellular SAR optimization of chemical series toward more potent and selective small molecules, upon MMoA deconvolution through a diverse array of target identification techniques (Table 4.2), it positions medicinal chemistry and disease biology very favorably both to indentify leads and candidates and to validate unprecedented targets. 

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