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2000
Volume 12, Issue 3
  • ISSN: 0929-8665
  • E-ISSN: 1875-5305

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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/content/journals/ppl/10.2174/0929866053587110
2005-04-01
2025-05-24
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/content/journals/ppl/10.2174/0929866053587110
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  • Article Type:
    Review Article
Keyword(s): amylase; binding segment; inhibitor; linker; tendamistat
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