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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 anddoi:10.1016/j.drudis.2013.10.018 pmid:24184433 pmcid:PMC4004703 fatcat:jsofekpezbdhtctkb3savhdome
more »... GPCRs. Here, we discuss how DREADDs can be used as novel tools for drug discovery and development.
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
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, anddoi:10.1016/j.ceb.2013.11.006 pmid:24680430 pmcid:PMC3971376 fatcat:mn3c4gy53famdn2bnqwwuemz6i
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.
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
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
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
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
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
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
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
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
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
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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