43 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
Discovery of a novel small molecule agonist scaffold for the APJ receptor.
Rti International
Discovery and Structure-Activity Relationship of a Bioactive Fragment of ELABELA that Modulates Vascular and Cardiac Functions.
University of Sherbrooke
C-Terminal modifications of apelin-13 significantly change ligand binding, receptor signaling, and hypotensive action.
University of Sherbrooke
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.
Novartis Institutes For Biomedical Research
Identifying structural determinants of potency for analogs of apelin-13: integration of C-terminal truncation with structure-activity.
Rti International
Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor.
Sanford-Burnham Medical Research Institute
Synthesis and characterization of an orally bioavailable small molecule agonist of the apelin receptor.
Rti International
Design and preparation of N-linked hydroxypyridine-based APJ agonists.
Bristol-Myers Squibb Research & Early Development
Pyrazole Agonist of the Apelin Receptor Improves Symptoms of Metabolic Syndrome in Mice.
Rti International
Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.
Bristol Myers Squibb
Identification of 6-hydroxy-5-phenyl sulfonylpyrimidin-4(1H)-one APJ receptor agonists.
Bristol-Myers Squibb
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
University of Sherbrooke
Structure-Activity Relationship and Bioactivity of Short Analogues of ELABELA as Agonists of the Apelin Receptor.
University of Sherbrooke
PEGylated and Acylated Elabela Analogues Show Enhanced Receptor Binding, Prolonged Stability, and Remedy of Acute Kidney Injury.
Huazhong University of Science & Technology
Optimizing PEG-Extended Apelin Analogues as Cardioprotective Drug Leads: Importance of the KFRR Motif and Aromatic Head Group for Improved Physiological Activity.
University of Alberta
Identification of potent pyrazole based APELIN receptor (APJ) agonists.
Rti International
Discovery and SAR of aryl hydroxy pyrimidinones as potent small molecule agonists of the GPCR APJ.
Bristol-Myers Squibb Research and Development
Plasma kallikrein cleaves and inactivates apelin-17: Palmitoyl- and PEG-extended apelin-17 analogs as metabolically stable blood pressure-lowering agents.
University of Alberta
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Shanghaitech University
Synthetic Modification within the"RPRL" Region of Apelin Peptides: Impact on Cardiovascular Activity and Stability to Neprilysin and Plasma Degradation.
University of Alberta
A Systematic Exploration of Macrocyclization in Apelin-13: Impact on Binding, Signaling, Stability, and Cardiovascular Effects.
University of Sherbrooke
3-aryl- heteroaryl substituted 5-trifluoromethyl oxadiazoles as histonedeacetylase 6 (HDAC6) inhibitors
Merck Sharp & Dohme
Fused tricyclic ring derivatives as SRC homology-2 phosphatase inhibitors
Nikang Therapeutics
Benzothiazol compounds and methods using the same for treating neurodegenerative disorders
1St Biotherapeutics
N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as Wnt signaling modulators
Novartis
Structure of REV-ERBß ligand-binding domain bound to a porphyrin antagonist.
The Scripps Research Institute
The Parkinson disease-linked LRRK2 protein mutation I2020T stabilizes an active state conformation leading to increased kinase activity.
Harvard Neurodiscovery Center
New cholinesterase inhibitors for Alzheimer's disease: Structure Activity Studies (SARs) and molecular docking of isoquinolone and azepanone derivatives.
Universidade De Evora
Inhibition of small ubiquitin-like modifier enzymes with substituted pyrrolo[2,3-b]quinoxalines
City of Hope
Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.
Gsk