A NanoBRET-Based Binding Assay for Smoothened Allows Real-time Analysis of Ligand Binding and Distinction of Two Binding Sites for BODIPY-cyclopamine

Glasdegib: First Global Approval

(2019) Sheridan M. Hoy   DRUGS

A conserved molecular switch in Class F receptors regulates receptor activation and pathway selection

(2019) Shane C. Wright et al.   Nature Communications

A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor

(2019) Monica Bouzo-Lorenzo et al.   Purinergic Signalling

Structural insight into Class F receptors – What have we learnt regarding agonist‐induced activation?

(2019) Gunnar Schulte et al.   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

Biochemical mechanisms of vertebrate hedgehog signaling

(2019) Jennifer H. Kong et al.   DEVELOPMENT

Binding kinetics of ligands acting at GPCRs

(2019) David A. Sykes et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Cryo-EM structure of oxysterol-bound human Smoothened coupled to a heterotrimeric Gi

(2019) Xiaofeng Qi et al.   NATURE

Smoothened stimulation by membrane sterols drives Hedgehog pathway activity

(2019) Ishan Deshpande et al.   NATURE

Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor

(2019) Reggie Bosma et al.   Scientific Reports

Structures of vertebrate Patched and Smoothened reveal intimate links between cholesterol and Hedgehog signalling

(2019) Christiane Kowatsch et al.   CURRENT OPINION IN STRUCTURAL BIOLOGY

Co-Localization Strategy Unveils an Underside Binding Site in the Transmembrane Domain of Smoothened Receptor

(2019) Fang Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Basis of Smoothened Activation in Hedgehog Signaling

(2018) Pengxiang Huang et al.   CELL

Discovery of potent and novel smoothened antagonists via structure-based virtual screening and biological assays

(2018) Wenfeng Lu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

NanoBRET Approaches to Study Ligand Binding to GPCRs and RTKs

(2018) Leigh A. Stoddart et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells

(2018) Leigh A. Stoddart et al.   Scientific Reports

Homogeneous, real-time NanoBRET binding assays for the histamine H3 and H4 receptor on living cells

(2018) Tamara A.M. Mocking et al.   MOLECULAR PHARMACOLOGY

Structural Basis for Cholesterol Transport-like Activity of the Hedgehog Receptor Patched

(2018) Yunxiao Zhang et al.   CELL

Overcoming the emerging drug resistance of smoothened: an overview of small-molecule SMO antagonists with antiresistance activity

(2018) Heng Zhang et al.   Future Medicinal Chemistry

Cilia-Associated Oxysterols Activate Smoothened

(2018) David R. Raleigh et al.   MOLECULAR CELL

Cellular Cholesterol Directly Activates Smoothened in Hedgehog Signaling

(2016) Pengxiang Huang et al.   CELL

Posaconazole, a Second-Generation Triazole Antifungal Drug, Inhibits the Hedgehog Signaling Pathway and Progression of Basal Cell Carcinoma

(2016) B. Chen et al.   MOLECULAR CANCER THERAPEUTICS

I only have eye for ewe: the discovery of cyclopamine and development of Hedgehog pathway-targeting drugs

(2016) James K. Chen   NATURAL PRODUCT REPORTS

Structural basis of Smoothened regulation by its extracellular domains

(2016) Eamon F. X. Byrne et al.   NATURE

Endogenous B-ring oxysterols inhibit the Hedgehog component Smoothened in a manner distinct from cyclopamine or side-chain oxysterols

(2016) Navdar Sever et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor

(2015) Lucile Hoch et al.   FASEB JOURNAL

Application of BRET to monitor ligand binding to GPCRs

(2015) Leigh A Stoddart et al.   NATURE METHODS

Structural basis for Smoothened receptor modulation and chemoresistance to anticancer drugs

(2014) Chong Wang et al.   Nature Communications

Lipidic cubic phase injector facilitates membrane protein serial femtosecond crystallography

(2014) Uwe Weierstall et al.   Nature Communications

Oxysterols are allosteric activators of the oncoprotein Smoothened

(2012) Sigrid Nachtergaele et al.   Nature Chemical Biology

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

(2011) Haiyan Tao et al.   CHEMISTRY & BIOLOGY

Virtual Screening-Based Discovery and Mechanistic Characterization of the Acylthiourea MRT-10 Family as Smoothened Antagonists

(2010) F. Manetti et al.   MOLECULAR PHARMACOLOGY

International Union of Basic and Clinical Pharmacology. LXXX. The Class Frizzled Receptors

(2010) G. Schulte   PHARMACOLOGICAL REVIEWS

Evidence for Allosteric Interactions of Antagonist Binding to the Smoothened Receptor

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