48168-99-6Relevant articles and documents
Metabolically stable apelin-analogues, incorporating cyclohexylalanine and homoarginine, as potent apelin receptor activators
Fernandez, Kleinberg X.,Fischer, Conrad,Gheblawi, Mahmoud,Gottschalk, Samantha,Iturrioz, Xavier,Oudit, Gavin Y.,Vederas, John C.,Vu, Jennie,Wang, Wang,Llorens-Cortés, Catherine
, p. 1402 - 1413 (2021/11/11)
High blood pressure and consequential cardiovascular diseases are among the top causes of death worldwide. The apelinergic (APJ) system has emerged as a promising target for the treatment of cardiovascular issues, especially prevention of ischemia reperfusion (IR) injury after a heart attack or stroke. However, rapid degradation of the endogenous apelin peptides in vivo limits their use as therapeutic agents. Here, we study the effects of simple homologue substitutions, i.e. incorporation of non-canonical amino acids l-cyclohexylalanine (l-Cha) and l-homoarginine (l-hArg), on the proteolytic stability of pyr-1-apelin-13 and apelin-17 analogues. The modified 13-mers display up to 40 times longer plasma half-life than native apelin-13 and in preliminary in vivo assay show moderate blood pressure-lowering effects. The corresponding apelin-17 analogues show pronounced blood pressure-lowering effects and up to a 340-fold increase in plasma half-life compared to the native apelin-17 isoforms, suggesting their potential use in the design of metabolically stable apelin analogues to prevent IR injury. This journal is
Rational design and synthesis of unsaturated 2,5-dioxopiperazine derivatives as potential protein tyrosine kinase inhibitors
Li, Wen-Ren,Peng, Shao-Zheng
, p. 7373 - 7376 (2007/10/03)
The first general method for the synthesis of a library of trifunctionalized (Z)-3-alkylidene-2,5-piperazinediones as potential protein tyrosine kinase inhibitors from commercially available amino compounds, α- keto acids and aldehydes using a novel cyclization/cleavage strategy on solid support is described.
Synthesis of cyclosporine. Part II. Synthesis of Boc-D-Ala-MeLeu-MeLeu-MeVal-OH, a part of the peptide sequence of cyclosporine, by different strategic ways and synthesis of its isomers Boc-D-Ala-MeLeu-D-MeLeu-MeVal-OH, Boc-D-Ala-Meleu-D-MeLeu-D-MeVal-OH,
Wenger
, p. 2672 - 2702 (2007/10/02)
-