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DREADDs: novel tools for drug discovery and development

Hyeong-Min Lee, Patrick M. Giguere, Bryan L. Roth
2014 Drug Discovery Today  
Since the invention of the first designer receptors exclusively activated by designer drugs (DREADDs), these engineered G protein-coupled receptors (GPCRs) have been widely applied in investigations of biological processes and behaviors. DREADD technology has emerged as a powerful tool with great potential for drug discovery and development. DREADDs can facilitate the identification of druggable targets and enable researchers to explore the activities of novel drugs against both known and
more » ... GPCRs. Here, we discuss how DREADDs can be used as novel tools for drug discovery and development.
doi:10.1016/j.drudis.2013.10.018 pmid:24184433 pmcid:PMC4004703 fatcat:jsofekpezbdhtctkb3savhdome

Molecular control of δ-opioid receptor signalling

Gustavo Fenalti, Patrick M. Giguere, Vsevolod Katritch, Xi-Ping Huang, Aaron A. Thompson, Vadim Cherezov, Bryan L. Roth, Raymond C. Stevens
2014 Nature  
Trinh and M. Chu for help with baculovirus expression, G.W. Han for help with structure analysis and quality control review, E. Abola for help with sodium site analysis, A.  ...  (0.3 mM -1 M).  ...  Diffraction quality crystals of an average size of 50×10×3 µm were obtained within ~10 d in 31-34% (v/v) PEG 400, 0.095 to 0.12 M K/Na tartrate, 5% (v/v) ethylene glycol, 100 mM MES buffer at pH 6.1-6.2  ... 
doi:10.1038/nature12944 pmid:24413399 pmcid:PMC3931418 fatcat:txfzi46yfjcaxggufvcfr6hmii

Tuning up the right signal: chemical and genetic approaches to study GPCR functions

Patrick M Giguere, Wesley K Kroeze, Bryan L Roth
2014 Current Opinion in Cell Biology  
The G protein-coupled receptor (GPCR) family is among the most druggable families in the human proteome. GPCRs are involved in most physiological processes, and our ability to modulate their activity is a hallmark of modern pharmacology. The means by which the activity of GPCRs can be modulated have been expanded by emerging data and concepts in pharmacology, which has created new strategies for their control. These new approaches will lead to the generation of more potent, selective, and
more » ... ent pharmaceutics, while reducing inappropriate actions and adverse effects. Herein, we review and comment on some recent advances in chemical and genetic approaches to the profiling of GPCR function, as well as the validation of orphan GPCRs as potential therapeutic targets using engineered receptors.
doi:10.1016/j.ceb.2013.11.006 pmid:24680430 pmcid:PMC3971376 fatcat:mn3c4gy53famdn2bnqwwuemz6i

RETRACTED: Structure of the Parathyroid Hormone Receptor C Terminus Bound to the G-Protein Dimer Gβ1γ2

Christopher A. Johnston, Adam J. Kimple, Patrick M. Giguère, David P. Siderovski
2008 Structure  
Sondek and M. Cheever for Gb1 and Gg2 baculoviridae and Gb5/ RGS9 protein, D.  ...  2.5% PEG-400, 0.1 M HEPES [pH 6.8-7.0]).  ...  Surfaces were regenerated after each Gb 1 g 2 injection with a single 10 ml pulse of 0.5 M NaCl/0.025 M NaOH at 20 ml/min. Kinetic analyses were made by using BIAevaluation v3.0.  ... 
doi:10.1016/j.str.2008.04.010 pmid:18611381 pmcid:PMC2601695 fatcat:g7ki6db6jjgd5oaoqzybf2p6dy

Consistent and High-Frequency Identification of an Intra-Sample Genetic Variant of SARS-CoV-2 with Elevated Fusogenic Properties [article]

Lynda Rocheleau, Geneviève Laroche, Kathy Fu, Marceline Côté, Patrick M Giguère, Marc-André Langlois, Martin Pelchat
2020 bioRxiv   pre-print
The expression construct encoding SARS-CoV-2 M was generated by PCR amplification of the M gene from pLVX-EF1alpha-SARS-CoV-2-M-2xStrep-IRES-Puro (kind gift of Dr.  ...  Overexpression of M was also detected by immunoblotting and using an anti-M antibody (Rabbit anti-SARS Membrane protein, NOVUS).  ... 
doi:10.1101/2020.12.03.409714 fatcat:itothuoph5gorffeyuv5bklswq

Diversity-Oriented Synthesis of Diol-Based Peptidomimetics as Potential HIV Protease Inhibitors and Antitumor Agents

Paresh M. Vadhadiya, Marc-Alexandre Jean, Chahrazed Bouzriba, Thomas Tremblay, Patrick Lagüe, Sébastien Fortin, John Boukouvalas, Denis Giguère
2018 ChemBioChem  
The M.  ...  Hz, 1H), 2.79 (dd, J = 13.2, 5.9 Hz, 1H), 2.70 -2.62 (m, 1H), 2.61 -2.52 (m, 1H), 2.43 (s, 3H), 2.30 -2.24 (m, 2H), 2.03 -1.91 (m, 1H), 1.49 -1.40 (m, 2H), 1.36 -1.27 (m, 2H), 0.97 (d, J = 6.6 Hz,  ... 
doi:10.1002/cbic.201800247 pmid:29858881 fatcat:aueixfakxbauvcyrrpube5i3nu

Retraction Notice to: Structure of the Parathyroid Hormone Receptor C Terminus Bound to the G-Protein Dimer Gβ1γ2

Christopher A. Johnston, Adam J. Kimple, Patrick M. Giguère, David P. Siderovski
2011 Structure  
doi:10.1016/j.str.2011.07.010 pmid:21827955 pmcid:PMC3401078 fatcat:6hky576ogjbptk5x7t4abhfzmq

Heterotrimeric G-protein Signaling Is Critical to Pathogenic Processes in Entamoeba histolytica

Dustin E. Bosch, Adam J. Kimple, Robin E. Muller, Patrick M. Giguère, Mischa Machius, Francis S. Willard, Brenda R. S. Temple, David P. Siderovski, William A. Petri
2012 PLoS Pathogens  
M. Leippe, U. of Kiel, Germany).  ...  (B) Trophozoite lysates were subjected to western blotting with anti-amoebapore A (kind gift of M. Leippe, U. of Kiel, Germany), with actin serving as a loading control.  ... 
doi:10.1371/journal.ppat.1003040 pmid:23166501 pmcid:PMC3499586 fatcat:oxczrqtipvc43ch2sh6bj4ev2e

Patient-Oriented Research from the ISDM 2019 Conference: A Legacy Now More Relevant Than Ever

Patrick M. Archambault, Sabrina Guay-Bélanger, Véronique Gélinas, Anik Giguère, Claire Ludwig, Mame Awa Ndiaye, Kathy Kastner, Dawn Stacey, Nick Bansback, Gary Groot, France Légaré
2020 Patient  
doi:10.1007/s40271-020-00463-2 pmid:33063238 fatcat:2jq4w7iukrbxpbttqwdgqfqoz4

Optimization of 2-Phenylcyclopropylmethylamines as Selective Serotonin 2C Receptor Agonists and Their Evaluation as Potential Antipsychotic Agents

Jianjun Cheng, Patrick M. Giguère, Oluseye K. Onajole, Wei Lv, Arsen Gaisin, Hendra Gunosewoyo, Claire M. Schmerberg, Vladimir M. Pogorelov, Ramona M. Rodriguiz, Giulio Vistoli, William C. Wetsel, Bryan L. Roth (+1 others)
2015 Journal of Medicinal Chemistry  
2H), 4.31−4.20 (m, 2H), 3.53−3.48 (m, 1H), 2.84−2.78 (m, 1H), 1.96−1.92 (m, 1H), 1.46 (s, 9H), 1.10−1.05 (m, 1H), 1.02−0.98 (m, 1H), 0.88−0.82 (m, 1H). 13 C NMR (100 MHz, CDCl 3 ) δ 157.7 (d, J CF = 237.5  ...  2H), 6.76 (dd, J = 9.2, 2.8 Hz, 1H), 4.87−4.75 (m, 2H), 4.32−4.20 (m, 2H), 3.04−3.00 (m, 2H), 2.19−2.15 (m, 1H), 1.28−1.17 (m, 2H), 1.06−1.02 (m, 1H). 13 C NMR (100 MHz, CD 3 OD) δ 159.0 (d, J CF =  ... 
doi:10.1021/jm5019274 pmid:25633969 pmcid:PMC4834193 fatcat:uzkhe4wlnrgkddxf4l4ftdfgga

G-protein Signaling Modulator-3 Regulates Heterotrimeric G-protein Dynamics through Dual Association with Gβ and GαiProtein Subunits

Patrick M. Giguère, Geneviève Laroche, Emily A. Oestreich, David P. Siderovski
2011 Journal of Biological Chemistry  
M. Giguère, G. Laroche, and D. P.  ...  BRET was initiated by adding coelenterazine 400a at a final concentration of 5 M.  ...  Patrick M. Giguère, Geneviève Laroche, Emily A. Oestreich and David P.  ... 
doi:10.1074/jbc.m111.311712 pmid:22167191 pmcid:PMC3281645 fatcat:adux7ysbkbeirkqxpefayk34ki

G Protein Signaling Modulator-3 Inhibits the Inflammasome Activity of NLRP3

Patrick M. Giguère, Bryan J. Gall, Ejiofor A. D. Ezekwe, Geneviève Laroche, Brian K. Buckley, Chahnaz Kebaier, Justin E. Wilson, Jenny P. Ting, David P. Siderovski, Joseph A. Duncan
2014 Journal of Biological Chemistry  
Truax, M. Schneider, A. B. Rogers, M. Mühlbauer, B. R. Barker, W.-C. Chou, W. J. Brickey, I. C. Allen, C. Jobin, D. Ramsden, B. K. Davis, and J. P. Ting, manuscript in preparation.  ...  BRET was initiated by adding coelenterazine-400a at a final concentration of 5 M.  ... 
doi:10.1074/jbc.m114.578393 pmid:25271165 pmcid:PMC4246083 fatcat:tmolaq4m2fbszh3et22mkj5lxq

RNA interference screen for RGS protein specificity at muscarinic and protease-activated receptors reveals bidirectional modulation of signaling

Geneviève Laroche, Patrick M. Giguère, Bryan L. Roth, JoAnn Trejo, David P. Siderovski
2010 American Journal of Physiology - Cell Physiology  
M. Giguère), and infrastructure support from the NIMH Psychoactive Drug Screening Program (to B. L. Roth).  ...  1 , M 3 , and M 4 mAChR transcripts.  ...  vs. 1.05 M on control cells; Table S .2).  ... 
doi:10.1152/ajpcell.00441.2009 pmid:20573995 pmcid:PMC2944319 fatcat:x3crt2ho7rbzvdhywhhxkklvpi

Design and synthesis of (2-(5-chloro-2,2-dimethyl-2,3-dihydrobenzofuran-7-yl)cyclopropyl)methanamine as a selective serotonin 2C agonist

Jianjun Cheng, Patrick M. Giguere, Wei Lv, Bryan L. Roth, Alan P. Kozikowski
2015 Tetrahedron Letters  
acquired with recombinantly expressed human serotonin receptors in HEK-293 (5-HT 2A and 5-HT 2B ) and PO1C (5-HT 2C ) cell lines, fluorescence imaging plate reader (FLIPR) assay; "NA", no activity at 10 µM.  ... 
doi:10.1016/j.tetlet.2015.01.060 pmid:26120215 pmcid:PMC4479288 fatcat:dfn7oazhnnejtefeu5p42nlxii

A Non-Canonical Function of Gβ as a Subunit of E3 Ligase in Targeting GRK2 Ubiquitylation

Zhengyu Zha, Xiaoran Han, Matthew D. Smith, Yang Liu, Patrick M. Giguère, Dragana Kopanja, Pradip Raychaudhuri, David P. Siderovski, Kun-Liang Guan, Qun-Ying Lei, Yue Xiong
2015 Molecular Cell  
Primary rat cardiomyocytes were incubated in DMEM medium supplemented with 10% FBS, 8 mM glutamine, 25 mM glucose, penicillin/streptomycin and 100 µM Brdu.  ...  Gβ subunits are present in cells either as Gαβγ heterotrimeric complexes, or as Gβγ dimers during GPCR activation, but rarely exist as monomers (Giguere et al., 2012; Wan et al., 2012) .  ... 
doi:10.1016/j.molcel.2015.04.017 pmid:25982117 pmcid:PMC4458238 fatcat:3d54q2pdgjfwdgapovlz5z74ey
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