Search Results - "Krumm, Brian"
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Structure of a Hallucinogen-Activated Gq-Coupled 5-HT2A Serotonin Receptor
Published in Cell (17-09-2020)“…Hallucinogens like lysergic acid diethylamide (LSD), psilocybin, and substituted N-benzyl phenylalkylamines are widely used recreationally with psilocybin…”
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TRUPATH, an open-source biosensor platform for interrogating the GPCR transducerome
Published in Nature chemical biology (01-08-2020)“…G-protein-coupled receptors (GPCRs) remain major drug targets, despite our incomplete understanding of how they signal through 16 non-visual G-protein signal…”
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3
Molecular glues as potential GPCR therapeutics
Published in Biochemical pharmacology (01-10-2024)“…[Display omitted] “Molecular Glues” are defined as small molecules that can either be endogenous or synthetic which promote interactions between proteins at…”
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Molecular mechanism of biased signaling at the kappa opioid receptor
Published in Nature communications (11-03-2023)“…The κ-opioid receptor (KOR) has emerged as an attractive drug target for pain management without addiction, and biased signaling through particular pathways of…”
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Structural prerequisites for G-protein activation by the neurotensin receptor
Published in Nature communications (24-07-2015)“…We previously determined the structure of neurotensin receptor NTSR1 in an active-like conformation with six thermostabilizing mutations bound to the peptide…”
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Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor
Published in Cell (11-01-2018)“…The κ-opioid receptor (KOP) mediates the actions of opioids with hallucinogenic, dysphoric, and analgesic activities. The design of KOP analgesics devoid of…”
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Structure, function and pharmacology of human itch GPCRs
Published in Nature (London) (02-12-2021)“…The MRGPRX family of receptors (MRGPRX1–4) is a family of mas-related G-protein-coupled receptors that have evolved relatively recently 1 . Of these, MRGPRX2…”
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Nanobody-enabled monitoring of kappa opioid receptor states
Published in Nature communications (02-03-2020)“…Recent studies show that GPCRs rapidly interconvert between multiple states although our ability to interrogate, monitor and visualize them is limited by a…”
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Molecular basis for selective activation of DREADD-based chemogenetics
Published in Nature (London) (08-12-2022)“…Designer receptors exclusively activated by designer drugs (DREADDs) represent a powerful chemogenetic technology for the remote control of neuronal activity…”
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Structures of the human dopamine D3 receptor-Gi complexes
Published in Molecular cell (18-03-2021)“…The dopamine system, including five dopamine receptors (D1R–D5R), plays essential roles in the central nervous system (CNS), and ligands that activate dopamine…”
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Structural biology of the IL‐1 superfamily: Key cytokines in the regulation of immune and inflammatory responses
Published in Protein science (01-05-2014)“…Interleukin‐1 superfamily of cytokines (IL‐1, IL‐18, IL‐33) play key roles in inflammation and regulating immunity. The mechanisms of agonism and antagonism in…”
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Signaling snapshots of a serotonin receptor activated by the prototypical psychedelic LSD
Published in Neuron (Cambridge, Mass.) (05-10-2022)“…Serotonin (5-hydroxytryptamine [5-HT]) 5-HT2-family receptors represent essential targets for lysergic acid diethylamide (LSD) and all other psychedelic drugs…”
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Ligand and G-protein selectivity in the κ-opioid receptor
Published in Nature (London) (11-05-2023)“…The κ-opioid receptor (KOR) represents a highly desirable therapeutic target for treating not only pain but also addiction and affective disorders 1 . However,…”
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Structure and dynamics of a constitutively active neurotensin receptor
Published in Scientific reports (07-12-2016)“…Many G protein-coupled receptors show constitutive activity, resulting in the production of a second messenger in the absence of an agonist; and naturally…”
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Ligand recognition and allosteric modulation of the human MRGPRX1 receptor
Published in Nature chemical biology (01-04-2023)“…The human MAS-related G protein–coupled receptor X1 (MRGPRX1) is preferentially expressed in the small-diameter primary sensory neurons and involved in the…”
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Bitter taste receptor activation by cholesterol and an intracellular tastant
Published in Nature (London) (18-04-2024)“…Bitter taste sensing is mediated by type 2 taste receptors (TAS2Rs (also known as T2Rs)), which represent a distinct class of G-protein-coupled receptors 1 …”
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Identification of small molecule inhibitors of Interleukin-18
Published in Scientific reports (28-03-2017)“…Interleukin-18 (IL-18) is a pleiotropic pro-inflammatory cytokine belonging to the IL-1 superfamily. IL-18 plays an important role in host innate and adaptive…”
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Inactive and active state structures template selective tools for the human 5-HT5A receptor
Published in Nature structural & molecular biology (01-07-2022)“…Serotonin receptors are important targets for established therapeutics and drug development as they are expressed throughout the human body and play key roles…”
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Structural genomics of the human dopamine receptor system
Published in Cell research (01-08-2023)“…The dopaminergic system, including five dopamine receptors (D1R to D5R), plays essential roles in the central nervous system (CNS); and ligands that activate…”
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Author Correction: Bitter taste receptor activation by cholesterol and an intracellular tastant
Published in Nature (London) (13-06-2024)Get full text
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