Activation of Apoptosis in Vivo by a Hydrocarbon-Stapled BH3 Helix

By L. Walensky, A. Kung, I. Escher, T. Malia, Scott Barbuto, R. Wright, G. Wagner, G. Verdine, S. Korsmeyer. Science, 2004

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Role of Bcl-2 family proteins and caspases in the regulation of apoptosis (2011, background): “A number of therapeutic approaches are undergoing using an antisense RNA [208], various small molecules [209–218, 222, 223], and peptidic compounds [219–221, 224, 225] classified as potential therapeutics to target the pathway of apoptosis, as briefly summarized in Table 2.”
An inhibitor of Bcl-2 family proteins induces regression of solid tumours (2005, background): “ABT-737 by itself was cytotoxic against the t(14;18) chromosomal translocation-containing lymphoma cell lines RS11380, DoHH2 and SuDHL-4 (median effective concentration EC50 1⁄4 0.”
Apoptosis and Molecular Targeting Therapy in Cancer (2014, unknown): “, HA14-1; [103]) and BH3 peptidomimetics [106].”
Stapled α−helical peptide drug development: A potent dual inhibitor of MDM2 and MDMX for p53-dependent cancer therapy (2013, methodology): “To determine dissociation constants for peptide–protein interaction, afluorescencepolarization assay (FPA) was used inwhich 10 nMof the fluorescently labeled analog of the linear peptide ATSP-3848 (specifically, FAM-β-Ala-Leu-Thr-Phe-Glu-His-Tyr-Trp-AlaGln-Leu-Thr-Ser-NH2 [FAM-ATSP-3848]) was incuba”