The 1,3‐diyne linker as a rigid “i,i+7” staple for α‐helix stabilization: Stereochemistry at work |
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Authors: | Steven Verlinden Niels Geudens Kevin Van holsbeeck Morgane Mannes Jos C Martins Guido Verniest Steven Ballet |
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Institution: | Steven Verlinden,Niels Geudens,Kevin Van holsbeeck,Morgane Mannes,José C. Martins,Guido Verniest,Steven Ballet |
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Abstract: | Short alphahelical peptide sequences were stabilized through Glaser‐Hay couplings of propargylated l ‐ and/or d ‐serine residues at positions i and i+7. NMR analysis confirmed a full stabilization of the helical structure when a d ‐Ser (i), l ‐Ser (i+7) combination was applied. In case two l ‐Ser residues were involved in the cyclization, the helical conformation is disrupted outside the peptide's macrocycle. |
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Keywords: | constrained peptides Glaser‐Hay coupling helix stabilization peptide stapling |
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