Abstract
Peptide analogues of Tendamistat which include the most essential residues linked by novel w-amino acids (X,Y,Z: H2N-(CH2)n-CO2H, where n=2-10) were designed, synthesized (Ac-Tyr15-X-Trp18-Arg19-Tyr20-Y-Thr55-Z-Asp58- Gly59-Tyr60-Ile61-Gly62-NH2), and analyzed for α-amylase inhibitory activity. Native dipeptide spacers sometimes were left intact at X and Z. Analogues demonstrated competitive inhibition with Ki values ranging from 23 to 767 μM. 8- Aminooctanoic acid was the optimal linker at Y, while longer linkers were favored at the other positions.
Keywords: amylase, inhibitor, tendamistat, binding segment, linker
Protein & Peptide Letters
Title: Peptide Inhibitors of a-Amylase Based on Tendamistat: Development of Analogues with ϖ-Amino Acids Linking Critical Binding Segments
Volume: 12 Issue: 3
Author(s): Deborah L. Heyl, Shakila Tobwala, Leo Solomon Lucas, A. Dammika Nandanie, Rebecca W. Himm, Jennifer Kappler, Elizabeth J. Blaney, Jason Groom, Jeffrey Asbill, Jonathan K. Nzoma, Cara Jarosz,, Hanna Palamma and Stephen E. Schullery
Affiliation:
Keywords: amylase, inhibitor, tendamistat, binding segment, linker
Abstract: Peptide analogues of Tendamistat which include the most essential residues linked by novel w-amino acids (X,Y,Z: H2N-(CH2)n-CO2H, where n=2-10) were designed, synthesized (Ac-Tyr15-X-Trp18-Arg19-Tyr20-Y-Thr55-Z-Asp58- Gly59-Tyr60-Ile61-Gly62-NH2), and analyzed for α-amylase inhibitory activity. Native dipeptide spacers sometimes were left intact at X and Z. Analogues demonstrated competitive inhibition with Ki values ranging from 23 to 767 μM. 8- Aminooctanoic acid was the optimal linker at Y, while longer linkers were favored at the other positions.
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Heyl L. Deborah, Tobwala Shakila, Lucas Solomon Leo, Nandanie Dammika A., Himm W. Rebecca, Kappler Jennifer, Blaney J. Elizabeth, Groom Jason, Asbill Jeffrey, Nzoma K. Jonathan, Jarosz, Cara, Palamma Hanna and Schullery E. Stephen, Peptide Inhibitors of a-Amylase Based on Tendamistat: Development of Analogues with ϖ-Amino Acids Linking Critical Binding Segments, Protein & Peptide Letters 2005; 12 (3) . https://dx.doi.org/10.2174/0929866053587110
DOI https://dx.doi.org/10.2174/0929866053587110 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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