GPCR structure and function relationship: identification of a biased apelin receptor mutant

Pharmacogenomics of GPCR Drug Targets

(2018) Alexander S. Hauser et al.   CELL

Biased signalling: from simple switches to allosteric microprocessors

(2018) Jeffrey S. Smith et al.   NATURE REVIEWS DRUG DISCOVERY

Identification of essential genes for cancer immunotherapy

(2017) Shashank J. Patel et al.   NATURE

Trends in GPCR drug discovery: new agents, targets and indications

(2017) Alexander S. Hauser et al.   NATURE REVIEWS DRUG DISCOVERY

Structural Basis for Apelin Control of the Human Apelin Receptor

(2017) Yingli Ma et al.   STRUCTURE

An apelin receptor antagonist prevents pathological retinal angiogenesis with ischemic retinopathy in mice

(2017) Yuki Ishimaru et al.   Scientific Reports

Cardiac action of the first G protein biased small molecule apelin agonist

(2016) Cai Read et al.   BIOCHEMICAL PHARMACOLOGY

Allostery and Biased Agonism at Class B G Protein-Coupled Receptors

(2016) Denise Wootten et al.   CHEMICAL REVIEWS

Quantifying biased signaling in GPCRs using BRET-based biosensors

(2016) Yoon Namkung et al.   METHODS

Structure-based discovery of opioid analgesics with reduced side effects

(2016) Aashish Manglik et al.   NATURE

A randomized, phase 2 study investigating TRV130, a biased ligand of the μ-opioid receptor, for the intravenous treatment of acute pain

(2016) Eugene R. Viscusi et al.   PAIN

Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using enhanced bystander BRET

(2016) Yoon Namkung et al.   Nature Communications

NanoLuc Complementation Reporter Optimized for Accurate Measurement of Protein Interactions in Cells

(2015) Andrew S. Dixon et al.   ACS Chemical Biology

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

Apela Regulates Fluid Homeostasis by Binding to the APJ Receptor to Activate Gi Signaling

(2015) Cheng Deng et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural Basis for Ligand Recognition and Functional Selectivity at Angiotensin Receptor

(2015) Haitao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Quercetin Enhances Cisplatin Sensitivity of Human Osteosarcoma Cells by Modulating microRNA-217-KRAS Axis

(2015) Xian Zhang et al.   MOLECULES AND CELLS

Crystal structure of rhodopsin bound to arrestin by femtosecond X-ray laser

(2015) Yanyong Kang et al.   NATURE

Elucidation of G-protein and β-arrestin functional selectivity at the dopamine D2 receptor

(2015) Sean M. Peterson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Apelin, Elabela/Toddler, and biased agonists as novel therapeutic agents in the cardiovascular system

(2015) Peiran Yang et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Tyrosine 308 Is Necessary for Ligand-directed GsProtein-biased Signaling of β2-Adrenoceptor

(2014) Anthony Yiu-Ho Woo et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Identification of Serine 348 on the Apelin Receptor as a Novel Regulatory Phosphorylation Site in Apelin-13-induced G Protein-independent Biased Signaling

(2014) Xiaoyu Chen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Biased Agonism at G Protein-Coupled Receptors: The Promise and the Challenges-A Medicinal Chemistry Perspective

(2014) Jeremy Shonberg et al.   MEDICINAL RESEARCH REVIEWS

Molecular control of δ-opioid receptor signalling

(2014) Gustavo Fenalti et al.   NATURE

Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers

(2014) David G. Soergel et al.   PAIN

Molecular signatures of G-protein-coupled receptors

(2013) A. J. Venkatakrishnan et al.   NATURE

APJ acts as a dual receptor in cardiac hypertrophy

(2012) Maria Cecilia Scimia et al.   NATURE

Crystal Structures of a Stabilized β1-Adrenoceptor Bound to the Biased Agonists Bucindolol and Carvedilol

(2012) Tony Warne et al.   STRUCTURE

Identification of Essential Cannabinoid-binding Domains

(2011) Joong-Youn Shim et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Crystal structure of the β2 adrenergic receptor–Gs protein complex

(2011) Søren G. F. Rasmussen et al.   NATURE

OPM database and PPM web server: resources for positioning of proteins in membranes

(2011) Mikhail A. Lomize et al.   NUCLEIC ACIDS RESEARCH

Distinct Phosphorylation Sites on the  2-Adrenergic Receptor Establish a Barcode That Encodes Differential Functions of  -Arrestin

(2011) K. N. Nobles et al.   Science Signaling

Study of a structurally similar kappa opioid receptor agonist and antagonist pair by molecular dynamics simulations

(2010) Michal Kolinski et al.   JOURNAL OF MOLECULAR MODELING