Metabolically stable apelin-analogues, incorporating cyclohexylalanine and homoarginine, as potent apelin receptor activators
Kleinberg X. Fernandez, Conrad Fischer, Jennie Vu, Mahmoud Gheblawi, Wang Wang, Samantha Gottschalk, Xavier Iturrioz, Catherine Llorens‐Cortés, Gavin Y. Oudit, John C. Vederas
Abstract
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.
Topics & Concepts
ApelinReceptorChemistryPharmacologyBiologyInternal medicineBiochemistryMedicineApelin-related biomedical researchLipid metabolism and disordersCardiovascular, Neuropeptides, and Oxidative Stress Research