BI-32169 / Boehringer Ingelheim - LARVOL DELTA

Structural signatures of the class III lasso peptide BI-32169 and the branched-cyclic topoisomers using trapped ion mobility spectrometry-mass spectrometry and tandem mass spectrometry. (PubMed, Anal Bioanal Chem) - "Experiments reducing and alkylating the disulfide bond of BI-32169 showed that the lasso structure is preserved and heat stable and the associated conformational changes provide new insights about the role of the disulfide bond in the inhibitory activity against the human glucagon receptor. Graphical abstract ᅟ."

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Cryptand-imidazolium supported total synthesis of the lasso peptide BI-32169 and its d-enantiomer. (PubMed, Chem Commun (Camb)) - "Herein, a cryptand-imidazolium complex is designed as a multi-linker support and applied in the chemical synthesis of the lasso peptide BI-32169. Furthermore, the chiral switching of the support and the introduction of d-amino acids enable the synthesis of the d-enantiomer of BI-32169, which shows not only a strong glucagon receptor antagonist activity, but also a much higher enzymatic stability compared to the l-lasso peptide."

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