Stapled peptide assays

Verdine and coworkers reported their first success with Bcl-2 family proteins using a stapled peptide analog of the proapoptotic Bid BH3 domain [37]. The hydrocarbon-crosslinked peptide was shown to bind Bcl-xL at the same binding site as wild-type Bid BH3 and with increased affinity. Importantly, the hydrocarbon crosslink rendered the stapled peptide cell permeable, where the wild-type peptide was not. In cell-based assays, stapled Bid BH3 was shown to sensitize cancer cells to Bax mediated apoptosis. In mice with leukemia xenografts, stapled Bid BH3 treatment consistently suppressed tumor growth. 

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

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