Biased Ligands for Better Cardiovascular Drugs

Modulation of HDL metabolism by the niacin receptor GPR109A in mouse hepatocytes

(2010) Xiaoyu Li et al.   BIOCHEMICAL PHARMACOLOGY

Being mindful of seven-transmembrane receptor ‘guests’ when assessing agonist selectivity

(2010) Terry Kenakin   BRITISH JOURNAL OF PHARMACOLOGY

GPR120 Is an Omega-3 Fatty Acid Receptor Mediating Potent Anti-inflammatory and Insulin-Sensitizing Effects

(2010) Da Young Oh et al.   CELL

The role of conformational ensembles of seven transmembrane receptors in functional selectivity

(2010) Nagarajan Vaidehi et al.   CURRENT OPINION IN PHARMACOLOGY

Third Generation Antipsychotic Drugs: Partial Agonism or Receptor Functional Selectivity?

(2010) Richard Mailman et al.   CURRENT PHARMACEUTICAL DESIGN

Angiotensin II revisited: new roles in inflammation, immunology and aging

(2010) Ariela Benigni et al.   EMBO Molecular Medicine

Differential Signaling of the Endogenous Agonists at the β2-Adrenergic Receptor

(2010) Susanne Reiner et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cardiorenal Actions of TRV120027, a Novel, β-Arrestin-Biased Ligand at the Angiotensin II Type I Receptor, in Healthy and Heart Failure Canines: A Novel Therapeutic Strategy for Acute Heart Failure

(2010) Guido Boerrigter et al.   JOURNAL OF CARDIAC FAILURE

β-Arrestin–dependent activation of Ca2+/calmodulin kinase II after β1–adrenergic receptor stimulation

(2010) Supachoke Mangmool et al.   JOURNAL OF CELL BIOLOGY

Functional Selectivity and Biased Receptor Signaling

(2010) T. Kenakin   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Selectively Engaging  -Arrestins at the Angiotensin II Type 1 Receptor Reduces Blood Pressure and Increases Cardiac Performance

(2010) J. D. Violin et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Quantitative Phosphoproteomics Dissection of Seven-transmembrane Receptor Signaling Using Full and Biased Agonists

(2010) Gitte L. Christensen et al.   MOLECULAR & CELLULAR PROTEOMICS

Quantification of Functional Selectivity at the Human  1A-Adrenoceptor

(2010) B. A. Evans et al.   MOLECULAR PHARMACOLOGY

Seven Transmembrane Receptors as Shapeshifting Proteins: The Impact of Allosteric Modulation and Functional Selectivity on New Drug Discovery

(2010) T. Kenakin et al.   PHARMACOLOGICAL REVIEWS

Global phosphorylation analysis of  -arrestin-mediated signaling downstream of a seven transmembrane receptor (7TMR)

(2010) K. Xiao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Kinase cascades and ligand-directed signaling at the kappa opioid receptor

(2010) Michael R. Bruchas et al.   PSYCHOPHARMACOLOGY

 -Arrestin-Biased Agonism of the Angiotensin Receptor Induced by Mechanical Stress

(2010) K. Rakesh et al.   Science Signaling

Therapeutic potential of β-arrestin- and G protein-biased agonists

(2010) Erin J. Whalen et al.   TRENDS IN MOLECULAR MEDICINE

The minor binding pocket: a major player in 7TM receptor activation

(2010) Mette M. Rosenkilde et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

β1-Adrenergic receptors stimulate cardiac contractility and CaMKII activation in vivo and enhance cardiac dysfunction following myocardial infarction

(2009) ByungSu Yoo et al.   AMERICAN JOURNAL OF PHYSIOLOGY-HEART AND CIRCULATORY PHYSIOLOGY

G protein-coupled receptor hetero-dimerization: contribution to pharmacology and function

(2009) Graeme Milligan   BRITISH JOURNAL OF PHARMACOLOGY

Role of protein kinase C in functional selectivity for desensitization at the µ-opioid receptor: from pharmacological curiosity to therapeutic potential

(2009) Susan L Ingram et al.   BRITISH JOURNAL OF PHARMACOLOGY

Dimerization in GPCR mobility and signaling

(2009) Martin J Lohse   CURRENT OPINION IN PHARMACOLOGY

The Current Status and Future Perspectives of Studies of Cannabinoid Receptor 1 Antagonists as Anti-Obesity Agents

(2009) Hyeon-Kyu Lee et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

β-Arrestin-2 Mediates Anti-apoptotic Signaling through Regulation of BAD Phosphorylation

(2009) Seungkirl Ahn et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

β-Arrestin1 mediates nicotinic acid–induced flushing, but not its antilipolytic effect, in mice

(2009) Robert W. Walters et al.   JOURNAL OF CLINICAL INVESTIGATION

Acute Heart Failure Syndromes

(2009) Mihai Gheorghiade et al.   JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY

Proteases Display Biased Agonism at Protease-Activated Receptors: Location matters!

(2009) A. Russo et al.   MOLECULAR INTERVENTIONS

GPCR homomers and heteromers: A better choice as targets for drug development than GPCR monomers?

(2009) Vicent Casadó et al.   PHARMACOLOGY & THERAPEUTICS

Selective engagement of G protein coupled receptor kinases (GRKs) encodes distinct functions of biased ligands

(2009) D. A. Zidar et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Of Mice and Men

(2008) G.F. Watts et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Niacin Increases HDL by Reducing Hepatic Expression and Plasma Levels of Cholesteryl Ester Transfer Protein in APOE*3Leiden.CETP Mice

(2008) José W.A. van der Hoorn et al.   ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY

Membrane signalling complexes: Implications for development of functionally selective ligands modulating heptahelical receptor signalling

(2008) Graciela Piñeyro   CELLULAR SIGNALLING

Beta-Arrestin-Mediated Signaling in the Heart

(2008) Priyesh A. Patel et al.   CIRCULATION JOURNAL

β-Arrestins Regulate Atherosclerosis and Neointimal Hyperplasia by Controlling Smooth Muscle Cell Proliferation and Migration

(2008) Jihee Kim et al.   CIRCULATION RESEARCH

Niacin Extended-Release/Simvastatin

(2008) Mark Sanford et al.   DRUGS

Novel d-amino acid tetrapeptides produce potent antinociception by selectively acting at peripheral κ-opioid receptors,

(2008) Todd W. Vanderah et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

β-Arrestin-mediated Signaling Regulates Protein Synthesis

(2008) Scott M. DeWire et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Agonist-selective, Receptor-specific Interaction of Human P2YReceptors with β-Arrestin-1 and -2

(2008) Carsten Hoffmann et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Effects of a niacin receptor partial agonist, MK-0354, on plasma free fatty acids, lipids, and cutaneous flushing in humans

(2008) Eseng Lai et al.   Journal of Clinical Lipidology

3-(1H-Tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (MK-0354): A Partial Agonist of the Nicotinic Acid Receptor, G-Protein Coupled Receptor 109a, with Antilipolytic but No Vasodilatory Activity in Mice

(2008) Graeme Semple et al.   JOURNAL OF MEDICINAL CHEMISTRY

Nicotinic Acid Receptor Agonists

(2008) P. Douglas Boatman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Conformational Rearrangements and Signaling Cascades Involved in Ligand-Biased Mitogen-Activated Protein Kinase Signaling through the  1-Adrenergic Receptor

(2008) S. Galandrin et al.   MOLECULAR PHARMACOLOGY

Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders

(2008) P. Jeffrey Conn et al.   NATURE REVIEWS DRUG DISCOVERY

Physiological and pharmacological implications of beta-arrestin regulation

(2008) Cullen L. Schmid et al.   PHARMACOLOGY & THERAPEUTICS

Distinct conformational changes in  -arrestin report biased agonism at seven-transmembrane receptors

(2008) A. K. Shukla et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

 -Blockers alprenolol and carvedilol stimulate  -arrestin-mediated EGFR transactivation

(2008) I.-M. Kim et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Effects of Laropiprant on Nicotinic Acid-Induced Flushing in Patients With Dyslipidemia††A list of study investigators appears in the Appendix.

(2007) John F. Paolini et al.   AMERICAN JOURNAL OF CARDIOLOGY

Nicotinic Acid: Pharmacological Effects and Mechanisms of Action

(2007) Andreas Gille et al.   Annual Review of Pharmacology and Toxicology

Pharmacological Onomastics: What's in a name?

(2007) T P Kenakin   BRITISH JOURNAL OF PHARMACOLOGY