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DREADDs: novel tools for drug discovery and development
2014
Drug Discovery Today
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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
doi:10.1016/j.drudis.2013.10.018
pmid:24184433
pmcid:PMC4004703
fatcat:jsofekpezbdhtctkb3savhdome
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... GPCRs. Here, we discuss how DREADDs can be used as novel tools for drug discovery and development.
Molecular control of δ-opioid receptor signalling
2014
Nature
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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
2014
Current Opinion in Cell Biology
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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
doi:10.1016/j.ceb.2013.11.006
pmid:24680430
pmcid:PMC3971376
fatcat:mn3c4gy53famdn2bnqwwuemz6i
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... 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.
RETRACTED: Structure of the Parathyroid Hormone Receptor C Terminus Bound to the G-Protein Dimer Gβ1γ2
2008
Structure
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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]
2020
bioRxiv
pre-print
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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
2018
ChemBioChem
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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
2011
Structure
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Heterotrimeric G-protein Signaling Is Critical to Pathogenic Processes in Entamoeba histolytica
2012
PLoS Pathogens
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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
2020
Patient
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Optimization of 2-Phenylcyclopropylmethylamines as Selective Serotonin 2C Receptor Agonists and Their Evaluation as Potential Antipsychotic Agents
2015
Journal of Medicinal Chemistry
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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
2011
Journal of Biological Chemistry
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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
2014
Journal of Biological Chemistry
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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
2010
American Journal of Physiology - Cell Physiology
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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
2015
Tetrahedron Letters
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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
2015
Molecular Cell
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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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