Synthesis and biophysical characterization of stabilized alpha-helices of BCL-2 domains.
作者： Gregory H. Bird , Federico Bernal , Kenneth Pitter , Loren D. Walensky
DOI: 10.1016/S0076-6879(08)01622-4
关键词:
摘要: Rational design of compounds to mimic the functional domains BCL-2 family proteins requires chemical reproduction biologic complexity afforded by relatively large and folded surfaces homology (BH) domain peptide alpha-helices. Because intermolecular handshakes are so critical controlling cellular fate, we undertook development a toolbox peptidic ligands that harness natural potency specificity BH alpha-helices interrogate potentially medicate deregulated apoptotic pathways human disease. To overcome classic deficiencies reagents, including loss bioactive structure in solution, rapid proteolytic degradation vivo, impermeability, developed new class based on hydrocarbon stapling BH3 death peptides. Here describe synthesis Stabilized Alpha-Helices or SAHBs, analytical methods used characterize their secondary structure, stability, penetrance.
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