X-ray structures of endothelin ETB receptor bound to clinical antagonist bosentan and its analog

From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective

(2016) Christoph Boss et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Thermostabilization of the Human Endothelin Type B Receptor

(2016) Akiko Okuta et al.   JOURNAL OF MOLECULAR BIOLOGY

Activation mechanism of endothelin ETB receptor by endothelin-1

(2016) Wataru Shihoya et al.   NATURE

Crystal structure of the human OX2 orexin receptor bound to the insomnia drug suvorexant

(2014) Jie Yin et al.   NATURE

Molecular control of δ-opioid receptor signalling

(2014) Gustavo Fenalti et al.   NATURE

The 2.1 Å Resolution Structure of Cyanopindolol-Bound β1-Adrenoceptor Identifies an Intramembrane Na+ Ion that Stabilises the Ligand-Free Receptor

(2014) Jennifer L. Miller-Gallacher et al.   PLoS One

Distinct ETA Receptor Binding Mode of Macitentan As Determined by Site Directed Mutagenesis

(2014) John Gatfield et al.   PLoS One

Allosteric sodium in class A GPCR signaling

(2014) Vsevolod Katritch et al.   TRENDS IN BIOCHEMICAL SCIENCES

Processing of X-ray snapshots from crystals in random orientations

(2014) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Pulmonary arterial hypertension: a rare disease that encourages the development of multiple treatments

(2014) Peter Norman   Expert Opinion on Orphan Drugs

The Discovery of N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N′-propylsulfamide (Macitentan), an Orally Active, Potent Dual Endothelin Receptor Antagonist

(2012) Martin H. Bolli et al.   JOURNAL OF MEDICINAL CHEMISTRY

Translational research: A UK tissue bank for breast tumours

(2012) Alastair M. Thompson   NATURE

Structure of the agonist-bound neurotensin receptor

(2012) Jim F. White et al.   NATURE

High-resolution crystal structure of human protease-activated receptor 1

(2012) Cheng Zhang et al.   NATURE

TGFα shedding assay: an accurate and versatile method for detecting GPCR activation

(2012) Asuka Inoue et al.   NATURE METHODS

Slow Receptor Dissociation Kinetics Differentiate Macitentan from Other Endothelin Receptor Antagonists in Pulmonary Arterial Smooth Muscle Cells

(2012) John Gatfield et al.   PLoS One

Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions

(2012) W. Liu et al.   SCIENCE

A Fluorescence-Detection Size-Exclusion Chromatography-Based Thermostability Assay for Membrane Protein Precrystallization Screening

(2012) Motoyuki Hattori et al.   STRUCTURE

Regulation of Blood Pressure and Salt Homeostasis by Endothelin

(2011) Donald E. Kohan et al.   PHYSIOLOGICAL REVIEWS

XDS

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

PHENIX: a comprehensive Python-based system for macromolecular structure solution

(2010) Paul D. Adams et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

MolProbity: all-atom structure validation for macromolecular crystallography

(2009) Vincent B. Chen et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Crystallizing membrane proteins using lipidic mesophases

(2009) Martin Caffrey et al.   Nature Protocols

An ion-responsive motif in the second transmembrane segment of rhodopsin-like receptors

(2008) M. S. Parker et al.   AMINO ACIDS

Peptidomimetics, a synthetic tool of drug discovery

(2008) Josef Vagner et al.   CURRENT OPINION IN CHEMICAL BIOLOGY