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Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile

Kien Trân, Robin Van Den Hauwe, Xavier Sainsily, Pierre Couvineau, Jérôme Côté, Louise R. Simard, Marco Echevarria, Alexandre Murza, Alexandra Serre, Léa Théroux, Sabrina Saibi, Lounès Haroune, Jean‐Michel Longpré, Olivier Lesur, Mannix Auger‐Messier, Claude Spino, Michel Bouvier, Philippe Sarret, Steven Ballet, Éric Marsault

2021Journal of Medicinal Chemistry23 citationsDOIOpen Access PDF

Abstract

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Topics & Concepts

ChemistryPharmacokineticsTerminal (telecommunication)ApelinSide chainAmino acidPharmacologyBiochemistryStereochemistryReceptorOrganic chemistryTelecommunicationsPolymerComputer scienceMedicineApelin-related biomedical researchNuclear Receptors and SignalingCardiovascular, Neuropeptides, and Oxidative Stress Research
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile | Litcius