Diastereomers of Coibamide A Show Altered Sec61 Client Selectivity and Ligand-Dependent Activity against Patient-Derived Glioma Stem-like Cells
Daphne R. Mattos,
Willian das Neves,
Takashi Kitamura
et al.
Abstract:Coibamide A (CbA) is a cyanobacterial lariat depsipeptide
that
selectively inhibits multiple secreted and integral membrane proteins
from entering the endoplasmic reticulum secretory pathway through
binding the alpha subunit of the Sec61 translocon. As a complex peptide-based
macrocycle with 13 stereogenic centers, CbA is presumed to adopt a
conformationally restricted orientation in the ligand-bound state,
resulting in potent antitumor and antiangiogenic bioactivity. A stereochemical
structure–activity relati… Show more
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