Stapled peptide correlation

Stapled Peptide Affinity Evaluation and a-Helix Content Correlation 10.3.4.1 Surface Plasmon Resonance Binding Assays... 

Stapled Peptide Affinity and a-Helix Content Correlation... 

Stapled peptides are designed to increase the a-helix content in solution and are expected to produce higher affinity ligands compared to the natural peptide modulators. The following examples demonstrate this correlation, although it should be noted that peptide stapling does not always lead to an increase in affinity. 

Other noteworthy work focused on the biophysical and computational chemistry of stapled p53 peptide analogs of the SAH-p53-8 series (see compound 6) have shown a predictive correlation of a-helicity with experimental circular dichroism, and stapled p53 peptide binding to MDM2(X) further predicting direct contact between the hydrocarbon linker moiety of SAH-p53-8 (6) and the target protein. Importantly, such predictions were subsequently verified by the determination of an X-ray crystal structure of the stapled p53 peptide SAH-p53-8 bound to MDM2. Very recently,... 

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