Search Results - "Hall, Dawn L."
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Structural basis for the cooperative allosteric activation of the free fatty acid receptor GPR40
Published in Nature structural & molecular biology (01-07-2017)“…Crystal structures of hGPR40, a target for treatment of type 2 diabetes, bound to a partial and an allosteric agonist explain the binding cooperativity between…”
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Structures of active-state orexin receptor 2 rationalize peptide and small-molecule agonist recognition and receptor activation
Published in Nature communications (05-02-2021)“…Narcolepsy type 1 (NT1) is a chronic neurological disorder that impairs the brain’s ability to control sleep-wake cycles. Current therapies are limited to the…”
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Structural Basis of Human p70 Ribosomal S6 Kinase-1 Regulation by Activation Loop Phosphorylation
Published in The Journal of biological chemistry (12-02-2010)“…p70 ribosomal S6 kinase (p70S6K) is a downstream effector of the mTOR signaling pathway involved in cell proliferation, cell growth, cell-cycle progression,…”
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Synthesis and Evaluation of Heterocyclic Catechol Mimics as Inhibitors of Catechol-O-methyltransferase (COMT)
Published in ACS medicinal chemistry letters (12-03-2015)“…3-Hydroxy-4-pyridinones and 5-hydroxy-4-pyrimidinones were identified as inhibitors of catechol-O-methyltransferase (COMT) in a high-throughput screen. These…”
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Structure of Human Prostasin, a Target for the Regulation of Hypertension
Published in The Journal of biological chemistry (12-12-2008)“…Prostasin (also called channel activating protease-1 (CAP1)) is an extracellular serine protease implicated in the modulation of fluid and electrolyte…”
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Structural definition and substrate specificity of the S28 protease family: the crystal structure of human prolylcarboxypeptidase
Published in BMC structural biology (11-06-2010)“…The unique S28 family of proteases is comprised of the carboxypeptidase PRCP and the aminopeptidase DPP7. The structural basis of the different substrate…”
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Insights into activity and inhibition from the crystal structure of human O-GlcNAcase
Published in Nature chemical biology (01-06-2017)“…Crystallographic analysis of human O-GlcNAc hydrolase (hOGA) fragments containing the catalytic domain, including structures in complex with known inhibitors,…”
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Structure and Function of the Hypertension Variant A486V of G Protein-coupled Receptor Kinase 4
Published in The Journal of biological chemistry (14-08-2015)“…G-protein-coupled receptor (GPCR) kinases (GRKs) bind to and phosphorylate GPCRs, initiating the process of GPCR desensitization and internalization. GRK4 is…”
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Integration of Affinity Selection-Mass Spectrometry and Functional Cell-Based Assays to Rapidly Triage Druggable Target Space within the NF-κB Pathway
Published in Journal of biomolecular screening (01-07-2016)“…The primary objective of early drug discovery is to associate druggable target space with a desired phenotype. The inability to efficiently associate these…”
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Structure of apo, unactivated insulin-like growth factor-1 receptor kinase at 1.5 Å resolution
Published in Acta crystallographica. Section D, Biological crystallography. (01-10-2003)“…The crystal structure of the wild‐type unactivated kinase domain (IGFRK‐0P) of insulin‐like growth factor‐1 receptor has been reported previously at 2.7 Å…”
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Structural Basis for Selective Small Molecule Kinase Inhibition of Activated c-Met
Published in The Journal of biological chemistry (01-04-2011)“…The receptor tyrosine kinase c-Met is implicated in oncogenesis and is the target for several small molecule and biologic agents in clinical trials for the…”
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Characterization of Non-Nitrocatechol Pan and Isoform Specific Catechol-O-methyltransferase Inhibitors and Substrates
Published in ACS chemical neuroscience (15-02-2012)“…Reduced dopamine neurotransmission in the prefrontal cortex has been implicated as causal for the negative symptoms and cognitive deficit associated with…”
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Dissociation and association of the HIV-1 protease dimer subunits: Equilibria and rates
Published in Biochemistry (Easton) (11-01-1994)“…The kinetics and equilibrium properties were investigated for the interconversion between the active dimer of human immunodeficiency virus 1 (HIV-1) protease…”
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Crystal structure of the Apo, unactivated insulin-like growth factor-1 receptor kinase. Implication for inhibitor specificity
Published in The Journal of biological chemistry (11-10-2002)“…The x-ray structure of the unactivated kinase domain of insulin-like growth factor-1 receptor (IGFRK-0P) is reported here at 2.7 A resolution. IGFRK-0P is…”
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Biochemical and Structural Characterization of a Novel Class of Inhibitors of the Type 1 Insulin-like Growth Factor and Insulin Receptor Kinases
Published in Biochemistry (Easton) (12-07-2005)“…The type 1 insulin-like growth factor receptor (IGF-1R) is often overexpressed on tumor cells and is believed to play an important role in…”
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Expression, purification and crystallization of human prolylcarboxypeptidase
Published in Acta crystallographica. Section F, Structural biology and crystallization communications (01-06-2010)“…Prolylcarboxypeptidase (PrCP) is a lysosomal serine carboxypeptidase that cleaves a variety of C‐terminal amino acids adjacent to proline and has been…”
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Active Human Cytomegalovirus Protease Is a Dimer (∗)
Published in The Journal of biological chemistry (29-03-1996)“…The quaternary state of the human cytomegalovirus (hCMV) protease has been analyzed in relation to its catalysis of peptide hydrolysis. Based on results…”
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Activation of the Herpes Simplex Virus Type 1 Protease
Published in The Journal of biological chemistry (29-09-1995)“…The catalytic efficiency of the mature HSV-1 protease has been examined as a function of solvent composition. With the peptide substrate HTYLQASEKFKMWG-amide,…”
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Protein expression plasmids produced rapidly: streamlining cloning protocols and robotic handling
Published in Assay and drug development technologies (01-12-2005)“…As many processes in the preclinical drug discovery process become highly parallel, the need to also produce a large number of different proteins in parallel…”
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Crystal Structure of the Apo, Unactivated Insulin-like Growth Factor-1 Receptor Kinase
Published in The Journal of biological chemistry (11-10-2002)“…The x-ray structure of the unactivated kinase domain of insulin-like growth factor-1 receptor (IGFRK-0P) is reported here at 2.7 Å resolution. IGFRK-0P is…”
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