312624-65-0Relevant articles and documents
Synthetic Modification within the rPRL Region of Apelin Peptides: Impact on Cardiovascular Activity and Stability to Neprilysin and Plasma Degradation
McKinnie, Shaun M. K.,Wang, Wang,Fischer, Conrad,McDonald, Tyler,Kalin, Kevin R.,Iturrioz, Xavier,Llorens-Cortes, Catherine,Oudit, Gavin Y.,Vederas, John C.
, p. 6408 - 6427 (2017)
Apelin is an important mammalian peptide hormone with a range of physiological roles, especially in the cardiovascular system. The apelinergic system is a promising target for treatment of disease, but this remains to be realized due to rapid proteolysis of apelin-derived peptides by proteases, including neprilysin (NEP). The synthetic analogues modified within the NEP degradation site ( RPRL motif) showed improved in vitro proteolytic stability while maintaining receptor-binding affinities, with three candidate peptides retaining full cardiovascular activities for potential therapeutic application. Many such analogues proved physiologically inactive even with relatively conservative modifications, highlighting the importance of this region for full agonist activity of this peptide hormone.
Synthetic method of (2S)-2-N-fluorene methoxycarbonyl amino-2,4-dimethyl valerate
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, (2019/03/08)
The invention relates to a synthetic method of (2S)-2-N-fluorene methoxycarbonyl amino-2,4-dimethyl valerate. According to the synthetic method, the technical problems that potassium cyanide is highlytoxic, and the enzymatic resolution yield is low in an