Search Results - "Kendall, Debra A."
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Signal peptidase I: Cleaving the way to mature proteins
Published in Protein science (01-01-2012)“…Signal peptidase I (SPase I) is critical for the release of translocated preproteins from the membrane as they are transported from a cytoplasmic site of…”
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Ligand-specific endocytic dwell times control functional selectivity of the cannabinoid receptor 1
Published in Nature communications (01-08-2014)“…G protein-coupled receptors (GPCRs) are the major transducers of external stimuli and key therapeutic targets in many pathological conditions. When activated…”
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Anti-inflammatory and antinociceptive effects of the selective cannabinoid CB2 receptor agonist ABK5
Published in Journal of pharmacological sciences (01-04-2021)“…Cannabinoid receptors are a potential target for anti-inflammatory and pain therapeutics. There are two subtypes, CB1 and CB2, and Δ9-tetrahydrocannabinol…”
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Optimization of Chemical Functionalities of Indole-2-carboxamides To Improve Allosteric Parameters for the Cannabinoid Receptor 1 (CB1)
Published in Journal of medicinal chemistry (10-04-2014)“…5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (1; ORG27569) is a prototypical allosteric modulator for the cannabinoid type 1…”
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Characterization of Subtype Selective Cannabinoid CB2 Receptor Agonists as Potential Anti-Inflammatory Agents
Published in Pharmaceuticals (Basel, Switzerland) (19-04-2021)“…Activation of the CB2 receptor has been shown to have anti-inflammatory and antinociceptive effects without causing psychoactive effects. Previously, we…”
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Structural Optimization of the Diarylurea PSNCBAM-1, an Allosteric Modulator of Cannabinoid Receptor 1
Published in Current therapeutic research (01-01-2020)“…•PSNCBAM-1 is an allosteric modulator of the cannabinoid receptor 1.•Derivatives of PSNCBAM-1 were made, to reduce the total rings in the structure.•Several…”
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Dual role of the second extracellular loop of the cannabinoid receptor 1: ligand binding and receptor localization
Published in Molecular pharmacology (01-10-2009)“…The seven transmembrane alpha-helices of G protein-coupled receptors (GPCRs) are the hallmark of this superfamily. Intrahelical interactions are critical to…”
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Mapping of the SecA Signal Peptide Binding Site and Dimeric Interface by Using the Substituted Cysteine Accessibility Method
Published in Journal of Bacteriology (01-10-2013)“…SecA is an ATPase nanomotor critical for bacterial secretory protein translocation. Secretory proteins carry an amino-terminal signal peptide that is…”
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Defining the Escherichia coli SecA Dimer Interface Residues through In Vivo Site-Specific Photo-Cross-Linking
Published in Journal of Bacteriology (01-06-2013)“…The motor protein SecA is a core component of the bacterial general secretory (Sec) pathway and is essential for cell viability. Despite evidence showing that…”
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Cannabinoid Receptors in the Central Nervous System: Their Signaling and Roles in Disease
Published in Frontiers in cellular neuroscience (04-01-2017)“…The identification and cloning of the two major cannabinoid (CB and CB ) receptors together with the discovery of their endogenous ligands in the late 80s and…”
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Hydrophobic Residues in Helix 8 of Cannabinoid Receptor 1 Are Critical for Structural and Functional Properties
Published in Biochemistry (Easton) (26-01-2010)“…In addition to the heptahelical transmembrane domain shared by all G protein-coupled receptors (GPCRs), many class A GPCRs adopt a helical domain, termed helix…”
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Modulation of CB1 cannabinoid receptor by allosteric ligands: Pharmacology and therapeutic opportunities
Published in Neuropharmacology (15-09-2017)“…Cannabinoid pharmacology has been intensely studied because of cannabis’ pervasive medicinal and non-medicinal uses as well as for the therapeutic potential of…”
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Oligomeric states of the SecA and SecYEG core components of the bacterial Sec translocon
Published in Biochimica et biophysica acta (01-01-2007)“…Many proteins synthesized in the cytoplasm ultimately function in non-cytoplasmic locations. In Escherichia coli, the general secretory (Sec) pathway…”
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Membrane assembly of the cannabinoid receptor 1: impact of a long N-terminal tail
Published in Molecular pharmacology (01-09-2003)“…The human cannabinoid receptor 1 (CB1) belongs to the G protein-coupled receptor (GPCR) family. Among the members of GPCR family, it has an exceptionally long…”
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Allosteric Modulator ORG27569 Induces CB1 Cannabinoid Receptor High Affinity Agonist Binding State, Receptor Internalization, and Gi Protein-independent ERK1/2 Kinase Activation
Published in The Journal of biological chemistry (06-04-2012)“…The cannabinoid receptor 1 (CB1), a member of the class A G protein-coupled receptor family, is expressed in brain tissue where agonist stimulation primarily…”
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Minireview: From the Bench, Toward the Clinic: Therapeutic Opportunities for Cannabinoid Receptor Modulation
Published in Molecular endocrinology (Baltimore, Md.) (01-06-2015)“…The effects of cannabinoids have been known for centuries and over the past several decades two G protein-coupled receptors, CB1 and CB2, that are responsible…”
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Allosteric modulators restore orthosteric agonist binding to mutated CB1 receptors
Published in Journal of pharmacy and pharmacology (01-01-2020)“…Abstract Objectives To determine if diminished orthosteric agonist binding due to mutations in extracellular loops 1 or 2 of the cannabinoid receptor 1 (CB1)…”
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Translational potential of allosteric modulators targeting the cannabinoid CB1 receptor
Published in Acta pharmacologica Sinica (01-03-2019)“…The cannabinoid type-1 (CB 1 ) receptor, a G-protein-coupled receptor, is an attractive target for drug discovery due to its involvement in many physiological…”
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Translational potential of allosteric modulators targeting the cannabinoid CB 1 receptor
Published in Acta pharmacologica Sinica (01-03-2019)“…The cannabinoid type-1 (CB ) receptor, a G-protein-coupled receptor, is an attractive target for drug discovery due to its involvement in many physiological…”
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Allosteric modulators of cannabinoid receptor 1: developing compounds for improved specificity
Published in Drug metabolism reviews (02-01-2018)“…The cannabinoid receptor 1 (CB 1 ) is a G protein-coupled receptor (GPCR) that is located primarily in the central nervous system. CB 1 is a therapeutic target…”
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