Search Results - "Bohn, M"
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Fulfilling the Promise of "Biased" G Protein-Coupled Receptor Agonism
Published in Molecular pharmacology (01-09-2015)“…The fact that over 30% of current pharmaceuticals target heptahelical G protein-coupled receptors (GPCRs) attests to their tractability as drug targets…”
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2
Toward Directing Opioid Receptor Signaling to Refine Opioid Therapeutics
Published in Biological psychiatry (1969) (01-01-2020)“…The mu opioid receptor (MOR) is a diversely regulated target for the alleviation of pain in the clinical setting. However, untoward side effects such as…”
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Crystal Structure of the Human Cannabinoid Receptor CB1
Published in Cell (20-10-2016)“…Cannabinoid receptor 1 (CB1) is the principal target of Δ9-tetrahydrocannabinol (THC), a psychoactive chemical from Cannabis sativa with a wide range of…”
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Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics
Published in Cell (16-11-2017)“…Biased agonism has been proposed as a means to separate desirable and adverse drug responses downstream of G protein-coupled receptor (GPCR) targets. Herein,…”
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Crystal Structure of the Human Cannabinoid Receptor CB2
Published in Cell (24-01-2019)“…The cannabinoid receptor CB2 is predominately expressed in the immune system, and selective modulation of CB2 without the psychoactivity of CB1 has therapeutic…”
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Crystal structures of agonist-bound human cannabinoid receptor CB1
Published in Nature (London) (27-07-2017)“…Crystal structures of the human cannabinoid receptor 1 (CB 1 ) bound to the agonists AM11542 and AM841 reveal notable structural rearrangements upon receptor…”
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Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-Gi Complex Structures
Published in Cell (20-02-2020)“…Human endocannabinoid systems modulate multiple physiological processes mainly through the activation of cannabinoid receptors CB1 and CB2. Their high sequence…”
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The role of beta-arrestin2 in the severity of antinociceptive tolerance and physical dependence induced by different opioid pain therapeutics
Published in Neuropharmacology (01-01-2011)“…Ligands acting at the same receptor can differentially activate distinct signal transduction pathways, which in turn, can have diverse functional consequences…”
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Community guidelines for GPCR ligand bias: IUPHAR review 32
Published in British journal of pharmacology (01-07-2022)“…GPCRs modulate a plethora of physiological processes and mediate the effects of one‐third of FDA‐approved drugs. Depending on which ligand activates a…”
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Zinc-Assisted Hydrodeoxygenation of Biomass-Derived 5-Hydroxymethylfurfural to 2,5-Dimethylfuran
Published in ChemSusChem (01-11-2014)“…2,5‐Dimethylfuran (DMF), a promising cellulosic biofuel candidate from biomass derived intermediates, has received significant attention because of its low…”
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11
Functional selectivity of GPCR signaling in animals
Published in Current opinion in cell biology (01-04-2014)“…Graphical abstract…”
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Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria
Published in Science signaling (29-11-2016)“…Agonists targeting the kappa opioid receptor (KOR) have been promising therapeutic candidates because of their efficacy for treating intractable itch and…”
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An evaluation of Mg/Ca, Sr/Ca, and Ba/Ca ratios as environmental proxies in aragonite bivalve shells
Published in Chemical geology (09-03-2015)“…The influence of salinity and water chemistry on Mg/Ca, Sr/Ca, and Ba/Ca ratios in the aragonitic shells of the Manila clam was investigated. Clams were reared…”
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14
U–Th stratigraphy of a cold seep carbonate crust
Published in Chemical geology (15-03-2009)“…On continental margins, oxidation of methane-rich fluids from the sediment often leads to formation of authigenic carbonate pavements on the seafloor. The…”
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Desensitization of G protein-coupled receptors and neuronal functions
Published in Annual review of neuroscience (01-01-2004)“…G protein-coupled receptors (GPCRs) have proven to be the most highly favorable class of drug targets in modern pharmacology. Over 90% of nonsensory GPCRs are…”
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Agonist-directed signaling of the serotonin 2A receptor depends on β-arrestin-2 interactions in vivo
Published in Proceedings of the National Academy of Sciences - PNAS (22-01-2008)“…Visual and auditory hallucinations accompany certain neuropsychiatric disorders, such as schizophrenia, and they also can be induced by the use or abuse of…”
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Comparison of morphine, oxycodone and the biased MOR agonist SR-17018 for tolerance and efficacy in mouse models of pain
Published in Neuropharmacology (01-03-2021)“…The mu opioid receptor-selective agonist, SR-17018, preferentially activates GTPγS binding over βarrestin2 recruitment in cellular assays, thereby…”
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Development of Functionally Selective, Small Molecule Agonists at Kappa Opioid Receptors
Published in The Journal of biological chemistry (20-12-2013)“…The kappa opioid receptor (KOR) is widely expressed in the CNS and can serve as a means to modulate pain perception, stress responses, and affective reward…”
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Angiogenesis imaging study using interim [18F] RGD-K5 PET/CT in patients with lymphoma undergoing chemotherapy: preliminary evidence
Published in EJNMMI research (12-04-2021)“…Background Our aim was to measure the impact of two cycles of standard chemotherapy on tumoural neoangiogenesis by [ 18 F] fluorine arginine-glycine-aspartic…”
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Structure of an affinity-matured inhibitory recombinant fab against urokinase plasminogen activator reveals basis of potency and specificity
Published in Biochimica et biophysica acta. Proteins and proteomics (01-02-2021)“…Affinity maturation of U33, a recombinant Fab inhibitor of uPA, was used to improve the affinity and the inhibitory effect compared to the parental Fab…”
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