Tools for GPCR drug discovery

AT1R-CB1R heteromerization reveals a new mechanism for the pathogenic properties of angiotensin II

(2011) Raphael Rozenfeld et al.   EMBO JOURNAL

Structure of the human histamine H1 receptor complex with doxepin

(2011) Tatsuro Shimamura et al.   NATURE

Crystal structure of the β2 adrenergic receptor–Gs protein complex

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

Comparing Label-Free Biosensors for Pharmacological Screening With Cell-Based Functional Assays

(2010) Matthew F. Peters et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Exploring a role for heteromerization in GPCR signalling specificity

(2010) Raphael Rozenfeld et al.   BIOCHEMICAL JOURNAL

Ligand-Based Peptide Design and Combinatorial Peptide Libraries to Target G Protein-Coupled Receptors

(2010) Christian W. Gruber et al.   CURRENT PHARMACEUTICAL DESIGN

G Protein Coupled Receptors - In Silico Drug Discovery and Design

(2010) I. Sela et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Label-free whole-cell assays: expanding the scope of GPCR screening

(2010) Clay W Scott et al.   DRUG DISCOVERY TODAY

Structures of the CXCR4 Chemokine GPCR with Small-Molecule and Cyclic Peptide Antagonists

(2010) B. Wu et al.   SCIENCE

Structure of the Human Dopamine D3 Receptor in Complex with a D2/D3 Selective Antagonist

(2010) E. Y. T. Chien et al.   SCIENCE

High content screening: seeing is believing

(2010) Fabian Zanella et al.   TRENDS IN BIOTECHNOLOGY

Receptor heteromerization and drug discovery

(2010) Raphael Rozenfeld et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Europium-labeled GTP as a general nonradioactive substitute for [35S]GTPγS in high-throughput G protein studies

(2009) Alexey Koval et al.   ANALYTICAL BIOCHEMISTRY

Improved donor/acceptor BRET couples for monitoring β-arrestin recruitment to G protein-coupled receptors

(2009) Maud Kamal et al.   Biotechnology Journal

Enhanced Selectivity Screening of GPCR Ligands Using a Label-Free Cell Based Assay Technology

(2009) Ryan McGuinness et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

G Protein-Coupled Receptors: Target-Based In Silico Screening

(2009) Hanoch Senderowitz et al.   CURRENT PHARMACEUTICAL DESIGN

Lipid G Protein-coupled Receptor Ligand Identification Using β-Arrestin PathHunter™ Assay

(2009) Hong Yin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A 100K well screen for a muscarinic receptor using the Epic®label-free system – a reflection on the benefits of the label-free approach to screening seven-transmembrane receptors

(2009) K. Dodgson et al.   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

Discovery of New GPCR Biology: One Receptor Structure at a Time

(2009) Michael A. Hanson et al.   STRUCTURE

Evaluation of Dynamic Mass Redistribution Technology for Pharmacological Studies of Recombinant and Endogenously Expressed G Protein-Coupled Receptors

(2008) Paul H. Lee et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

A 1,536-Well [35S]GTPγS Scintillation Proximity Binding Assay for Ultra-High-Throughput Screening of an Orphan Gαi-Coupled GPCR

(2008) Eric N. Johnson et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Scintillation Proximity Assays in High-Throughput Screening

(2008) J. Fraser Glickman et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Photoproteins: Important New Tools in Drug Discovery

(2008) Richard M. Eglen et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies: application to GPCR oligomerization

(2008) Damien Maurel et al.   NATURE METHODS

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

(2008) V.-P. Jaakola et al.   SCIENCE