Signalling bias in new drug discovery: detection, quantification and therapeutic impact
出版年份 2013 全文链接
标题
Signalling bias in new drug discovery: detection, quantification and therapeutic impact
作者
关键词
-
出版物
NATURE REVIEWS DRUG DISCOVERY
Volume 12, Issue 3, Pages 205-216
出版商
Springer Nature
发表日期
2013-02-15
DOI
10.1038/nrd3954
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注意:仅列出部分参考文献,下载原文获取全部文献信息。- Modeling of Bias for the Analysis of Receptor Signaling in Biochemical Systems
- (2012) Larry S. Barak et al. BIOCHEMISTRY
- TRV120027, a Novel β-Arrestin Biased Ligand at the Angiotensin II Type I Receptor, Unloads the Heart and Maintains Renal Function When Added to Furosemide in Experimental Heart Failure
- (2012) Guido Boerrigter et al. Circulation-Heart Failure
- Synthesis and Characterization of Novel 2-Amino-3-benzoylthiophene Derivatives as Biased Allosteric Agonists and Modulators of the Adenosine A1 Receptor
- (2012) Celine Valant et al. JOURNAL OF MEDICINAL CHEMISTRY
- Where have all the active receptor states gone?
- (2012) H Ongun Onaran et al. Nature Chemical Biology
- Biased Signaling Pathways in 2-Adrenergic Receptor Characterized by 19F-NMR
- (2012) J. J. Liu et al. SCIENCE
- A Simple Method for Quantifying Functional Selectivity and Agonist Bias
- (2011) Terry Kenakin et al. ACS Chemical Neuroscience
- Biased signalling and allosteric machines: new vistas and challenges for drug discovery
- (2011) Terry P Kenakin BRITISH JOURNAL OF PHARMACOLOGY
- Cardiorenal Actions of TRV120027, a Novel ß-Arrestin–Biased Ligand at the Angiotensin II Type I Receptor, in Healthy and Heart Failure Canines
- (2011) Guido Boerrigter et al. Circulation-Heart Failure
- Positive and Negative Allosteric Modulators Promote Biased Signaling at the Calcium-Sensing Receptor
- (2011) Anna E. Davey et al. ENDOCRINOLOGY
- The Antidepressant Desipramine Is an Arrestin-biased Ligand at the α2A-Adrenergic Receptor Driving Receptor Down-regulationin Vitroandin Vivo
- (2011) Christopher Cottingham et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Quantifying Ligand Bias at Seven-Transmembrane Receptors
- (2011) S. Rajagopal et al. MOLECULAR PHARMACOLOGY
- Structure of a nanobody-stabilized active state of the β2 adrenoceptor
- (2011) Søren G. F. Rasmussen et al. NATURE
- Crystal structure of the β2 adrenergic receptor–Gs protein complex
- (2011) Søren G. F. Rasmussen et al. NATURE
- Meningococcus Hijacks a β2-Adrenoceptor/β-Arrestin Pathway to Cross Brain Microvasculature Endothelium
- (2010) Mathieu Coureuil et al. CELL
- Identification of Orthosteric and Allosteric Site Mutations in M2Muscarinic Acetylcholine Receptors That Contribute to Ligand-selective Signaling Bias
- (2010) Karen J. Gregory et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- A Novel Biased Allosteric Compound Inhibitor of Parturition Selectively Impedes the Prostaglandin F2α-mediated Rho/ROCK Signaling Pathway
- (2010) Eugénie Goupil et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- 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
- -Opioid Receptors: Correlation of Agonist Efficacy for Signalling with Ability to Activate Internalization
- (2010) J. McPherson et al. MOLECULAR PHARMACOLOGY
- Allosteric Ligands of the Glucagon-Like Peptide 1 Receptor (GLP-1R) Differentially Modulate Endogenous and Exogenous Peptide Responses in a Pathway-Selective Manner: Implications for Drug Screening
- (2010) C. Koole et al. MOLECULAR PHARMACOLOGY
- Prediction of Functionally Selective Allosteric Interactions at an M3 Muscarinic Acetylcholine Receptor Mutant Using Saccharomyces cerevisiae
- (2010) G. D. Stewart et al. MOLECULAR PHARMACOLOGY
- Allosteric modulation of G protein-coupled receptors: A pharmacological perspective
- (2010) Peter Keov et al. NEUROPHARMACOLOGY
- 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
- β-Arrestin1 mediates nicotinic acid–induced flushing, but not its antilipolytic effect, in mice
- (2009) Robert W. Walters et al. JOURNAL OF CLINICAL INVESTIGATION
- Genetic Deletion of p90 Ribosomal S6 Kinase 2 Alters Patterns of 5-Hydroxytryptamine2A Serotonin Receptor Functional Selectivity
- (2009) R. T. Strachan et al. MOLECULAR PHARMACOLOGY
- Conformational Toggle Switches Implicated in Basal Constitutive and Agonist-Induced Activated States of 5-Hydroxytryptamine-4 Receptors
- (2009) L. P. Pellissier et al. MOLECULAR PHARMACOLOGY
- A -Arrestin-Biased Agonist of the Parathyroid Hormone Receptor (PTH1R) Promotes Bone Formation Independent of G Protein Activation
- (2009) D. Gesty-Palmer et al. Science Translational Medicine
- Kinetics of G-protein-coupled receptor signals in intact cells
- (2008) M J Lohse et al. BRITISH JOURNAL OF PHARMACOLOGY
- Membrane Type 1 Matrix Metalloproteinase Induces Epithelial-to-Mesenchymal Transition in Prostate Cancer
- (2008) Jian Cao et al. JOURNAL OF BIOLOGICAL CHEMISTRY
- Molecular determinants of angiotensin II type 1 receptor functional selectivity
- (2008) Mark Aplin et al. JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY
- Selectivity of Agonists for the Active State of M1 to M4 Muscarinic Receptor Subtypes
- (2008) K. W. Figueroa et al. JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
- Fluorescence Resonance Energy Transfer Analysis of 2a-Adrenergic Receptor Activation Reveals Distinct Agonist-Specific Conformational Changes
- (2008) A. Zurn et al. MOLECULAR PHARMACOLOGY
- Discovery and Characterization of Novel Allosteric Potentiators of M1 Muscarinic Receptors Reveals Multiple Modes of Activity
- (2008) J. E. Marlo et al. MOLECULAR PHARMACOLOGY
- 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
- Estimation of Relative Microscopic Affinity Constants of Agonists for the Active State of the Receptor in Functional Studies on M2 and M3 Muscarinic Receptors
- (2008) J. A. Tran et al. MOLECULAR PHARMACOLOGY
- On the analysis of ligand-directed signaling at G protein-coupled receptors
- (2008) Frederick J. Ehlert NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
- Agonist-directed signaling of the serotonin 2A receptor depends on -arrestin-2 interactions in vivo
- (2008) C. L. Schmid et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- -Arrestin-1 mediates glucagon-like peptide-1 signaling to insulin secretion in cultured pancreatic cells
- (2008) N. Sonoda et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Unique agonist-bound cannabinoid CB1 receptor conformations indicate agonist specificity in signaling
- (2007) Teodora Georgieva et al. EUROPEAN JOURNAL OF PHARMACOLOGY
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