Abstract
Peptide analogs of tendamistat were synthesized and analyzed for α-amylase inhibitory activity. The pKa of the N-terminal tyrosine was modified by incorporation of ring-substituted analogs, which alters hydrogen bonding capacity. Ki values ranging from 70 to 524 μM generally increased with increasing pKa, indicating a necessity for H-bond donor ability.
Keywords: a-amylase, inhibitor, tendamistat, pka, hydrogen bonding, structure-activity relationship
Protein & Peptide Letters
Title: Variation of pKa in the N-Terminal Tyrosine Side Chain in Octapeptide Analogs of Tendamistat Influences α-Amylase Inhibition
Volume: 14 Issue: 5
Author(s): D. L. Heyl, B. Sethi, A. Rogalski, C. E. Bowen, M. Lawrence, L. Beitler, E. Harning, A. Hancer, S. Sreekumar and S. Fernandes
Affiliation:
Keywords: a-amylase, inhibitor, tendamistat, pka, hydrogen bonding, structure-activity relationship
Abstract: Peptide analogs of tendamistat were synthesized and analyzed for α-amylase inhibitory activity. The pKa of the N-terminal tyrosine was modified by incorporation of ring-substituted analogs, which alters hydrogen bonding capacity. Ki values ranging from 70 to 524 μM generally increased with increasing pKa, indicating a necessity for H-bond donor ability.
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Cite this article as:
Heyl L. D., Sethi B., Rogalski A., Bowen E. C., Lawrence M., Beitler L., Harning E., Hancer A., Sreekumar S. and Fernandes S., Variation of pKa in the N-Terminal Tyrosine Side Chain in Octapeptide Analogs of Tendamistat Influences α-Amylase Inhibition, Protein & Peptide Letters 2007; 14 (5) . https://dx.doi.org/10.2174/092986607780782867
DOI https://dx.doi.org/10.2174/092986607780782867 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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