Search Results - "HENNE, Kirk R"
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High-Throughput Liquid Chromatography-Tandem Mass Spectrometry Quantification of Glycosaminoglycans as Biomarkers of Mucopolysaccharidosis II
Published in International journal of molecular sciences (30-07-2020)“…We recently developed a blood-brain barrier (BBB)-penetrating enzyme transport vehicle (ETV) fused to the lysosomal enzyme iduronate 2-sulfatase (ETV:IDS) and…”
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2
Anti-PCSK9 antibody pharmacokinetics and low-density lipoprotein-cholesterol pharmacodynamics in nonhuman primates are antigen affinity-dependent and exhibit limited sensitivity to neonatal Fc receptor-binding enhancement
Published in The Journal of pharmacology and experimental therapeutics (01-04-2015)“…Proprotein convertase subtilisin/kexin type 9 (PCSK9) has emerged as an attractive therapeutic target for cardiovascular disease. Monoclonal antibodies (mAbs)…”
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3
Iduronate-2-sulfatase transport vehicle rescues behavioral and skeletal phenotypes in a mouse model of Hunter syndrome
Published in JCI insight (08-10-2021)“…Mucopolysaccharidosis type II (MPS II) is a lysosomal storage disorder caused by deficiency of the iduronate-2-sulfatase (IDS) enzyme, resulting in cellular…”
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4
Bioactivation of 4-Ipomeanol by CYP4B1: Adduct Characterization and Evidence for an Enedial Intermediate
Published in Chemical research in toxicology (01-05-2005)“…4-Ipomeanol (IPO) is a pneumotoxin that is bioactivated to a reactive intermediate that binds to DNA and other cellular macromolecules. Despite over 30 years…”
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5
Brain delivery of therapeutic proteins using an Fc fragment blood-brain barrier transport vehicle in mice and monkeys
Published in Science translational medicine (27-05-2020)“…Effective delivery of protein therapeutics to the central nervous system (CNS) has been greatly restricted by the blood-brain barrier (BBB). We describe the…”
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6
Molecular architecture determines brain delivery of a transferrin receptor-targeted lysosomal enzyme
Published in The Journal of experimental medicine (07-03-2022)“…Delivery of biotherapeutics across the blood-brain barrier (BBB) is a challenge. Many approaches fuse biotherapeutics to platforms that bind the transferrin…”
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7
Discovery and in Vivo Evaluation of (S)‑N‑(1-(7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)‑9H‑purin-6-amine (AMG319) and Related PI3Kδ Inhibitors for Inflammation and Autoimmune Disease
Published in Journal of medicinal chemistry (08-01-2015)“…The development and optimization of a series of quinolinylpurines as potent and selective PI3Kδ kinase inhibitors with excellent physicochemical properties are…”
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BIOACTIVATION OF THE NONTRICYCLIC ANTIDEPRESSANT NEFAZODONE TO A REACTIVE QUINONE-IMINE SPECIES IN HUMAN LIVER MICROSOMES AND RECOMBINANT CYTOCHROME P450 3A4
Published in Drug metabolism and disposition (01-02-2005)“…The therapeutic benefits of the antidepressant nefazodone have been hampered by several cases of acute hepatotoxicity/liver failure. Although the mechanism of…”
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9
Metabolic activation of the nontricyclic antidepressant trazodone to electrophilic quinone-imine and epoxide intermediates in human liver microsomes and recombinant P4503A4
Published in Chemico-biological interactions (30-06-2005)“…Therapy with the antidepressant trazodone has been associated with several cases of idiosyncratic hepatotoxicity. While the mechanism of hepatotoxicity remains…”
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10
A comprehensive listing of bioactivation pathways of organic functional groups
Published in Current drug metabolism (01-06-2005)“…The occurrence of idiosyncratic adverse drug reactions during late clinical trials or after a drug has been released can lead to a severe restriction in its…”
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11
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme
Published in Drug metabolism and disposition (01-07-2012)“…CYP3A4-mediated biotransformation of…”
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12
Bioactivation of a Novel 2-Methylindole-Containing Dual Chemoattractant Receptor-Homologous Molecule Expressed on T-Helper Type-2 Cells/D-Prostanoid Receptor Antagonist Leads to Mechanism-Based CYP3A Inactivation: Glutathione Adduct Characterization and Prediction of In Vivo Drug-Drug Interaction
Published in Drug metabolism and disposition (01-05-2010)“…The 2-methyl substituted indole, 2MI [2-(4-(4-(2,4-dichlorophenylsulfonamido)-2-methyl-1H-indol-5-yloxy)-3-methoxyphenyl)acetic acid] is a potent dual…”
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13
Iduronate-2-sulfatase transport vehicle rescues behavioral and skeletal phenotypes in a mouse model of Hunter syndrome
Published in JCI insight (08-10-2021)Get full text
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14
A comparison of substrate dynamics in human CYP2E1 and CYP2A6
Published in Biochemical and biophysical research communications (26-01-2007)“…Considering the dynamic nature of CYPs, methods that reveal information about substrate and enzyme dynamics are necessary to generate predictive models. To…”
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15
Covalent Linkage of Prosthetic Heme to CYP4 Family P450 Enzymes
Published in Biochemistry (Easton) (30-10-2001)“…An extensive body of research on the structural properties of cytochrome P450 enzymes has established that these proteins possess a b-type heme prosthetic…”
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16
Covalent Heme Binding to CYP4B1 via Glu310 and a Carbocation Porphyrin Intermediate
Published in Biochemistry (Easton) (22-04-2003)“…Recently we found that CYP4B1, and several other members of the CYP4 family of enzymes, are covalently linked to their prosthetic heme group through an ester…”
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17
Enzymatic Determinants of the Substrate Specificity of CYP2C9: Role of B‘−C Loop Residues in Providing the π-Stacking Anchor Site for Warfarin Binding
Published in Biochemistry (Easton) (16-03-1999)“…Previous modeling efforts have suggested that coumarin ligand binding to CYP2C9 is dictated by electrostatic and π-stacking interactions with complementary…”
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18
Genotyping and site-directed mutagenesis of a cytochrome P450 meander Pro-X-Arg motif critical to CYP4B1 catalysis
Published in Toxicology and applied pharmacology (15-01-2003)“…CYP4B1 isoforms from rodents and other common laboratory animals are involved in the bioactivation of a range of protoxins, including 2-aminofluorene,…”
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Rescue of a lysosomal storage disorder caused by Grn loss of function with a brain penetrant progranulin biologic
Published in Cell (02-09-2021)“…GRN mutations cause frontotemporal dementia (GRN-FTD) due to deficiency in progranulin (PGRN), a lysosomal and secreted protein with unclear function. Here, we…”
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20
Active Site Characteristics of CYP4B1 Probed with Aromatic Ligands
Published in Biochemistry (Easton) (24-07-2001)“…The active site topography of rabbit CYP4B1 has been studied relative to CYP2B1 and CYP102 using a variety of aromatic probe substrates. Oxidation of the…”
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