Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs

Lipidic cubic phase injector facilitates membrane protein serial femtosecond crystallography

(2014) Uwe Weierstall et al.   Nature Communications

Discovery of NVP-LEQ506, a Second-Generation Inhibitor of Smoothened

(2013) Stefan Peukert et al.   ChemMedChem

Hedgehog Pathway Modulation by Multiple Lipid Binding Sites on the Smoothened Effector of Signal Response

(2013) Benjamin R. Myers et al.   DEVELOPMENTAL CELL

Structure of the human smoothened receptor bound to an antitumour agent

(2013) Chong Wang et al.   NATURE

Oxysterol binding to the extracellular domain of Smoothened in Hedgehog signaling

(2013) Daniel Nedelcu et al.   Nature Chemical Biology

Structural Basis for Molecular Recognition at Serotonin Receptors

(2013) C. Wang et al.   SCIENCE

Structural Features for Functional Selectivity at Serotonin Receptors

(2013) D. Wacker et al.   SCIENCE

Structural insights into the role of the Smoothened cysteine-rich domain in Hedgehog signalling

(2013) Rajashree Rana et al.   Nature Communications

Structure and function of the Smoothened extracellular domain in vertebrate Hedgehog signaling

(2013) Sigrid Nachtergaele et al.   eLife

Structure-Function of the G Protein–Coupled Receptor Superfamily

(2012) Vsevolod Katritch et al.   Annual Review of Pharmacology and Toxicology

Abstract 2819: Identification and characterization of a novel smoothened antagonist for the treatment of cancer with deregulated hedgehog signaling

(2012) Mark H. Bender et al.   CANCER RESEARCH

Hedgehog Partial Agonism Drives Warburg-like Metabolism in Muscle and Brown Fat

(2012) Raffaele Teperino et al.   CELL

Structure of the agonist-bound neurotensin receptor

(2012) Jim F. White et al.   NATURE

Crystal structure of the µ-opioid receptor bound to a morphinan antagonist

(2012) Aashish Manglik et al.   NATURE

The Hedgehog Signal Transduction Network

(2012) D. J. Robbins et al.   Science Signaling

Small Molecule Antagonists in Distinct Binding Modes Inhibit Drug-Resistant Mutant of Smoothened

(2011) Haiyan Tao et al.   CHEMISTRY & BIOLOGY

The structural basis for agonist and partial agonist action on a β1-adrenergic receptor

(2011) Tony Warne et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

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

Structure of an Agonist-Bound Human A2A Adenosine Receptor

(2011) F. Xu et al.   SCIENCE

Diversity and modularity of G protein-coupled receptor structures

(2011) Vsevolod Katritch et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Features and development ofCoot

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

Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance

(2010) Gerrit J. P. Dijkgraaf et al.   CANCER RESEARCH

GDC-0449—A potent inhibitor of the hedgehog pathway

(2009) Kirk D. Robarge et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Converse Conformational Control of Smoothened Activity by Structurally Related Small Molecules

(2009) Hongbo Yang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

1-Amino-4-benzylphthalazines as Orally Bioavailable Smoothened Antagonists with Antitumor Activity

(2009) Karen Miller-Moslin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Hedgehog-Gli Signaling Pathway Inhibitors as Anticancer Agents

(2009) Neeraj Mahindroo et al.   JOURNAL OF MEDICINAL CHEMISTRY

Evidence for Allosteric Interactions of Antagonist Binding to the Smoothened Receptor

(2009) C. M. Rominger et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Rastering strategy for screening and centring of microcrystal samples of human membrane proteins with a sub-10  m size X-ray synchrotron beam

(2009) V. Cherezov et al.   Journal of the Royal Society Interface

Crystallizing membrane proteins using lipidic mesophases

(2009) Martin Caffrey et al.   Nature Protocols

Inhibition of the Hedgehog Pathway in Advanced Basal-Cell Carcinoma

(2009) Daniel D. Von Hoff et al.   NEW ENGLAND JOURNAL OF MEDICINE

Hedgehog signal transduction by Smoothened: Pharmacologic evidence for a 2-step activation process

(2009) R. Rohatgi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex

(2009) X. J. Yao et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Smoothened Mutation Confers Resistance to a Hedgehog Pathway Inhibitor in Medulloblastoma

(2009) R. L. Yauch et al.   SCIENCE

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE

A Specific Cholesterol Binding Site Is Established by the 2.8 Å Structure of the Human β2-Adrenergic Receptor

(2008) Michael A. Hanson et al.   STRUCTURE