AzaGly-Appended Peptidomimetics Structurally Related to PTR6154 as Potential PKB/Akt Inhibitors
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Date
2017-04
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Publisher
Wiley
Abstract
Synthesis of AzaGly-appended peptidomimetics with improved biological and biochemical properties. Robust synthesis of azapeptide on solid support is demonstrated without noticeable hydantoin formation. The azapeptide derived from the GSK-3β substrate exhibited improved properties in terms of Akt kinase inhibitory activity and basal degradation, proteolytic degradation, conformation and binding affinities.
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Keywords
Pharmacy, Peptidomimetics, PKB/Akt Inhibitors