Journal ArticleDOI
Functional assays for screening GPCR targets
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TLDR
This work focuses on the design and implementation of high-throughput GPCR functional assays that allow the cost-effective screening of large compound libraries to identify novel drug candidates.About:
This article is published in Current Opinion in Biotechnology.The article was published on 2005-12-01. It has received 217 citations till now. The article focuses on the topics: Drug discovery.read more
Citations
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Illuminating G-Protein-Coupling Selectivity of GPCRs.
Asuka Inoue,Asuka Inoue,Francesco Raimondi,Francois Marie Ngako Kadji,Gurdeep Singh,Takayuki Kishi,Akiharu Uwamizu,Yuki Ono,Yuji Shinjo,Satoru Ishida,Nadia Arang,Kouki Kawakami,J. Silvio Gutkind,Junken Aoki,Robert B. Russell +14 more
TL;DR: This work systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique Gα subunit C termini, and identified sequence-based coupling specificity features, inside and outside the transmembrane domain, which were used to develop a coupling predictor that outperforms previous methods.
Journal ArticleDOI
Distinct profiles of functional discrimination among G proteins determine the actions of G protein–coupled receptors
Ikuo Masuho,Olga Ostrovskaya,Grant M. Kramer,Grant M. Kramer,Christopher D. Jones,Christopher D. Jones,Keqiang Xie,Kirill A. Martemyanov +7 more
TL;DR: The observations suggest that the diversity of the effects of GPCRs on cellular physiology may be determined by their differential engagement of multiple G proteins, coupling to which produces signals with varying signal magnitudes and activation kinetics, properties that may be exploited pharmacologically.
Journal ArticleDOI
Detection and Activity Profiling of Synthetic Cannabinoids and Their Metabolites with a Newly Developed Bioassay.
TL;DR: A new G-protein coupled receptor (GPCR) activation assay based on NanoLuc binary technology is developed and applied, and it is demonstrated that several major metabolites of these SCs retain their activity at cannabinoid receptors.
Journal ArticleDOI
Ins and outs of GPCR signaling in primary cilia.
TL;DR: An overview of GPCR signaling in primary cilia is provided, with main focus on the rhodopsin‐like and the smoothened/frizzled GPCRs.
Journal ArticleDOI
A Fluorescent Ligand-Binding Alternative Using Tag-lite® Technology
Jurriaan M. Zwier,Thomas Roux,Martin Cottet,Thierry Durroux,Stephanie Douzon,Sara Bdioui,Nathalie Gregor,Emmanuel Bourrier,Nadia Oueslati,Ludovic Nicolas,Norbert Tinel,Chloe Boisseau,Paul Yverneau,Fabienne Charrier-Savournin,Michel Fink,Eric Trinquet +15 more
TL;DR: The authors clearly demonstrate that the Tag-lite binding assay format can be successfully and reproducibly applied by using different cellular materials such as transient or stable recombinant cells lines expressing SNAP-tagged GPCR, and makes it completely suitable for HTS applications.
References
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Journal ArticleDOI
Substitution of three amino acids switches receptor specificity of Gq alpha to that of Gi alpha
TL;DR: It is proposed that a C-terminal turn, centred on this glycine, plays an important part in specifying receptor interactions of G proteins in the Gi/G0/Gz family.
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Insights into G protein structure, function, and regulation
Theresa M. Cabrera-Vera,Jurgen F. Vanhauwe,Tarita O. Thomas,Martina Medkova,Anita M. Preininger,Maria R. Mazzoni,Maria R. Mazzoni,Heidi E. Hamm,Heidi E. Hamm +8 more
TL;DR: An evolutionarily highly conserved group of molecules known as heterotrimeric guanine nucleotide-binding proteins (G proteins) are key determinants of the specificity and temporal characteristics of many signaling processes and are the topic of this review.
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Drug Design Strategies for Targeting G‐Protein‐Coupled Receptors
Thomas Klabunde,Gerhard Hessler +1 more
TL;DR: The crystal structure of rhodopsin provides the first three‐dimensional GPCR information, which now supports homology modeling studies and structure‐based drug design approaches within the G PCR target family, and may allow the mapping of the ligand binding to the receptor.
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A FlAsH-based FRET approach to determine G protein-coupled receptor activation in living cells.
Carsten Hoffmann,Guido M. Gaietta,Moritz Bünemann,Stephen R. Adams,Silke Oberdorff-Maass,Björn Behr,Jean-Pierre Vilardaga,Roger Y. Tsien,Mark H. Ellisman,Martin J. Lohse +9 more
TL;DR: FRET from CFP to FlAsH reports GPCR activation in living cells without disturbing receptor function and shows that the small size of the tetracysteine-biarsenical tag can be decisively advantageous.
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Receptor-Mediated Activation of Heterotrimeric G-Proteins in Living Cells
TL;DR: Construction of similar energy-transfer pairs of mammalian G-proteins should enable direct in situ mechanistic studies and applications such as drug screening and identifying ligands of newly found G-protein–coupled receptors.