Structure–activity relationship of novel macrocyclic biased apelin receptor agonists

Discovery and Structure–Activity Relationship of a Bioactive Fragment of ELABELA that Modulates Vascular and Cardiac Functions

(2016) Alexandre Murza et al.   JOURNAL OF MEDICINAL CHEMISTRY

New structural insights into the apelin receptor: identification of key residues for apelin binding

(2015) Romain Gerbier et al.   FASEB JOURNAL

Design, Characterization, and First-In-Human Study of the Vascular Actions of a Novel Biased Apelin Receptor Agonist

(2015) A. L. Brame et al.   HYPERTENSION

Regulation of the Apelinergic System and Its Potential in Cardiovascular Disease: Peptides and Small Molecules as Tools for Discovery

(2015) Sanju Narayanan et al.   JOURNAL OF MEDICINAL CHEMISTRY

C-Terminal Modifications of Apelin-13 Significantly Change Ligand Binding, Receptor Signaling, and Hypotensive Action

(2015) Alexandre Murza et al.   JOURNAL OF MEDICINAL CHEMISTRY

Elabela-Apelin Receptor Signaling Pathway is Functional in Mammalian Systems

(2015) Zhi Wang et al.   Scientific Reports

Biased ligands: pathway validation for novel GPCR therapeutics

(2014) David H Rominger et al.   CURRENT OPINION IN PHARMACOLOGY

Biased Signaling Favoring Giover β-Arrestin Promoted by an Apelin Fragment Lacking the C-terminal Phenylalanine

(2014) Emilie Ceraudo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure–Activity Relationship Studies toward the Discovery of Selective Apelin Receptor Agonists

(2014) Jean-François Margathe et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pyroglutamyl apelin-13 identified as the major apelin isoform in human plasma

(2013) Eugene Y. Zhen et al.   ANALYTICAL BIOCHEMISTRY

Structural features of the apelin receptor N-terminal tail and first transmembrane segment implicated in ligand binding and receptor trafficking

(2013) David N. Langelaan et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

ELABELA: A Hormone Essential for Heart Development Signals via the Apelin Receptor

(2013) Serene C. Chng et al.   DEVELOPMENTAL CELL

The apelin receptor APJ: journey from an orphan to a multifaceted regulator of homeostasis

(2013) Anne-Marie O'Carroll et al.   JOURNAL OF ENDOCRINOLOGY

APJ acts as a dual receptor in cardiac hypertrophy

(2012) Maria Cecilia Scimia et al.   NATURE

Differential  -Arrestin-Dependent Conformational Signaling and Cellular Responses Revealed by Angiotensin Analogs

(2012) B. Zimmerman et al.   Science Signaling

Discovery of a Competitive Apelin Receptor (APJ) Antagonist

(2011) N. J. Maximilian Macaluso et al.   ChemMedChem

Elucidation of the Structure-Activity Relationships of Apelin: Influence of Unnatural Amino Acids on Binding, Signaling, and Plasma Stability

(2011) Alexandre Murza et al.   ChemMedChem

The fate of the internalized apelin receptor is determined by different isoforms of apelin mediating differential interaction with β-arrestin

(2010) Dennis K. Lee et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Exploring the ‘RPRL’ Motif of Apelin-13 through Molecular Simulation and Biological Evaluation of Cyclic Peptide Analogues

(2010) N. J. Maximilian Macaluso et al.   ChemMedChem

Acute Cardiovascular Effects of Apelin in Humans

(2010) A.G. Japp et al.   CIRCULATION

Apelin Decreases Lipolysis via Gq, Gi, and AMPK-Dependent Mechanisms

(2010) Patrick Yue et al.   ENDOCRINOLOGY

The apelinergic system: a promising therapeutic target

(2010) Inês Falcão-Pires et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

By Interacting with the C-terminal Phe of Apelin, Phe255and Trp259in Helix VI of the Apelin Receptor Are Critical for Internalization

(2010) Xavier Iturrioz et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Solid-phase synthesis of short α-helices stabilized by the hydrogen bond surrogate approach

(2010) Anupam Patgiri et al.   Nature Protocols

Structural Insight into G-Protein Coupled Receptor Binding by Apelin†

(2009) David N. Langelaan et al.   BIOCHEMISTRY

G Protein-Coupled Receptor APJ and Its Ligand Apelin Act Downstream of Cripto to Specify Embryonic Stem Cells Toward the Cardiac Lineage Through Extracellular Signal-Regulated Kinase/p70S6 Kinase Signaling Pathway

(2009) Cristina D'Aniello et al.   CIRCULATION RESEARCH

Modulation of canine cardiac sodium current by Apelin

(2009) Caroline Chamberland et al.   JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY

Vascular Effects of Apelin In Vivo in Man

(2008) Alan G. Japp et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY