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  1. Article ; Online: Preclinical evaluation of [

    Bennacef, Idriss / Rubins, Daniel / Riffel, Kerry / Williams, Mangay / Posavec, Diane J / Holahan, Marie A / Purcell, Mona L / Haley, Hyking D / Wolf, Mary / Stachel, Shawn J / Lubbers, Laura S / Wesolowski, Gregg A / Duong, Le T / Hamill, Terence G / Evelhoch, Jeffrey L / Hostetler, Eric D

    Journal of labelled compounds & radiopharmaceuticals

    2020  Volume 64, Issue 4, Page(s) 159–167

    Abstract: The cathepsin K (CatK) enzyme is abundantly expressed in osteoclasts, and CatK inhibitors have been developed for the treatment of osteoporosis. In our effort to support discovery and clinical evaluations of a CatK inhibitor, we sought to discover a ... ...

    Abstract The cathepsin K (CatK) enzyme is abundantly expressed in osteoclasts, and CatK inhibitors have been developed for the treatment of osteoporosis. In our effort to support discovery and clinical evaluations of a CatK inhibitor, we sought to discover a radioligand to determine target engagement of the enzyme by therapeutic candidates using positron emission tomography (PET). L-235, a potent and selective CatK inhibitor, was labeled with carbon-11. PET imaging studies recording baseline distribution of [
    MeSH term(s) Animals ; Bone and Bones/diagnostic imaging ; Carbon Radioisotopes/chemistry ; Cathepsin K/antagonists & inhibitors ; Cysteine Proteinase Inhibitors/chemistry ; Drug Evaluation, Preclinical ; Female ; Ligands ; Macaca mulatta ; Osteoporosis/diagnostic imaging ; Positron Emission Tomography Computed Tomography/methods ; Protein Binding ; Rabbits ; Radiopharmaceuticals/adverse effects ; Radiopharmaceuticals/chemistry ; Radiopharmaceuticals/pharmacokinetics ; Tissue Distribution
    Chemical Substances Carbon Radioisotopes ; Cysteine Proteinase Inhibitors ; Ligands ; Radiopharmaceuticals ; Cathepsin K (EC 3.4.22.38)
    Language English
    Publishing date 2020-12-02
    Publishing country England
    Document type Journal Article
    ZDB-ID 196095-7
    ISSN 1099-1344 ; 0362-4803 ; 0022-2135
    ISSN (online) 1099-1344
    ISSN 0362-4803 ; 0022-2135
    DOI 10.1002/jlcr.3896
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: In Vivo Evaluation and Dosimetry Estimate for a High Affinity Affibody PET Tracer Targeting PD-L1.

    Rubins, Daniel J / Meng, Xiangjun / McQuade, Paul / Klimas, Michael / Getty, Krista / Lin, Shu-An / Connolly, Brett M / O'Malley, Stacey S / Haley, Hyking / Purcell, Mona / Gantert, Liza / Holahan, Marie / Lindgren, Joel / Eklund, Pär / Ekblad, Caroline / Frejd, Fredrik Y / Hostetler, Eric D / González Trotter, Dinko E / Evelhoch, Jeffrey L

    Molecular imaging and biology

    2020  Volume 23, Issue 2, Page(s) 241–249

    Abstract: Purpose: In vivo imaging of programmed death ligand 1 (PD-L1) during immunotherapy could potentially monitor changing PD-L1 expression and PD-L1 expression heterogeneity within and across tumors. Some protein constructs can be used for same-day positron ...

    Abstract Purpose: In vivo imaging of programmed death ligand 1 (PD-L1) during immunotherapy could potentially monitor changing PD-L1 expression and PD-L1 expression heterogeneity within and across tumors. Some protein constructs can be used for same-day positron emission tomography (PET) imaging. Previously, we evaluated the PD-L1-targeting Affibody molecule [
    Procedures: Z
    Results: Ex vivo biodistribution measurements showed that both tracers had > 25 fold higher accumulation in LOX tumors than SUDHL6 ([
    Conclusions: [
    MeSH term(s) Animals ; Antibodies, Monoclonal/administration & dosage ; Antibodies, Monoclonal/pharmacokinetics ; B7-H1 Antigen/immunology ; B7-H1 Antigen/metabolism ; Cell Line, Tumor ; Fluorine Radioisotopes ; Gallium Radioisotopes ; Humans ; Immunotherapy/methods ; Macaca mulatta ; Mice ; Molecular Imaging/methods ; Neoplasms/diagnostic imaging ; Neoplasms/drug therapy ; Neoplasms/immunology ; Neoplasms/metabolism ; Positron-Emission Tomography/methods ; Radiometry/methods ; Radiopharmaceuticals/administration & dosage ; Radiopharmaceuticals/pharmacokinetics ; Tissue Distribution ; Xenograft Model Antitumor Assays
    Chemical Substances Antibodies, Monoclonal ; B7-H1 Antigen ; CD274 protein, human ; Fluorine Radioisotopes ; Gallium Radioisotopes ; Radiopharmaceuticals ; Gallium-68 (98B30EPP5S) ; Fluorine-18 (GZ5I74KB8G)
    Language English
    Publishing date 2020-10-23
    Publishing country United States
    Document type Evaluation Study ; Journal Article
    ZDB-ID 2079160-4
    ISSN 1860-2002 ; 1536-1632
    ISSN (online) 1860-2002
    ISSN 1536-1632
    DOI 10.1007/s11307-020-01544-2
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: PET/CT Imaging of

    Li, Wenping / Wang, Yuchuan / Rubins, Daniel / Bennacef, Idriss / Holahan, Marie / Haley, Hyking / Purcell, Mona / Gantert, Liza / Hseih, SuChun / Judo, Michael / Seghezzi, Wolfgang / Zhang, Shuli / van der Veen, Elly L / Lub-de Hooge, Marjolijn N / de Vries, Elisabeth G E / Evelhoch, Jeffrey L / Klimas, Michael / Hostetler, Eric D

    Molecular imaging and biology

    2020  Volume 23, Issue 2, Page(s) 250–259

    Abstract: Purpose: Programmed cell death-1 receptor (PD-1) and its ligand (PD-L1) are the targets for immunotherapy in many cancer types. Although PD-1 blockade has therapeutic effects, the efficacy differs between patients. Factors contributing to this ... ...

    Abstract Purpose: Programmed cell death-1 receptor (PD-1) and its ligand (PD-L1) are the targets for immunotherapy in many cancer types. Although PD-1 blockade has therapeutic effects, the efficacy differs between patients. Factors contributing to this variability are PD-L1 expression levels and immune cells present in tumors. However, it is not well understood how PD-1 expression in the tumor microenvironment impacts immunotherapy response. Thus, imaging of PD-1-expressing immune cells is of interest. This study aims to evaluate the biodistribution of Zirconium-89 (
    Procedures: Pembrolizumab was conjugated with the tetrafluorophenol-N-succinyl desferal-Fe(III) ester (TFP-N-sucDf) and subsequently radiolabeled with
    Results: 89
    Conclusions: 89
    Trial registration: ClinicalTrials.gov Identifier: NCT02760225.
    MeSH term(s) Animals ; Antibodies, Monoclonal, Humanized/administration & dosage ; Antibodies, Monoclonal, Humanized/pharmacokinetics ; Antineoplastic Agents, Immunological/administration & dosage ; Antineoplastic Agents, Immunological/pharmacokinetics ; Female ; Immunotherapy/methods ; Macaca fascicularis ; Male ; Models, Animal ; Molecular Imaging/methods ; Neoplasms/diagnostic imaging ; Neoplasms/drug therapy ; Neoplasms/immunology ; Neoplasms/metabolism ; Positron Emission Tomography Computed Tomography/methods ; Programmed Cell Death 1 Receptor/immunology ; Programmed Cell Death 1 Receptor/metabolism ; Radioisotopes ; Tissue Distribution ; Zirconium
    Chemical Substances Antibodies, Monoclonal, Humanized ; Antineoplastic Agents, Immunological ; Programmed Cell Death 1 Receptor ; Radioisotopes ; Zirconium (C6V6S92N3C) ; pembrolizumab (DPT0O3T46P) ; Zirconium-89 (NTM296JU95)
    Language English
    Publishing date 2020-10-26
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2079160-4
    ISSN 1860-2002 ; 1536-1632
    ISSN (online) 1860-2002
    ISSN 1536-1632
    DOI 10.1007/s11307-020-01558-w
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Al

    Cleeren, Frederik / Lecina, Joan / Ahamed, Muneer / Raes, Geert / Devoogdt, Nick / Caveliers, Vicky / McQuade, Paul / Rubins, Daniel J / Li, Wenping / Verbruggen, Alfons / Xavier, Catarina / Bormans, Guy

    Theranostics

    2017  Volume 7, Issue 11, Page(s) 2924–2939

    Abstract: Positron emission tomography (PET) using radiolabeled biomolecules is a translational molecular imaging technology that is increasingly used in support of drug development. Current methods for radiolabeling biomolecules with fluorine-18 are laborious and ...

    Abstract Positron emission tomography (PET) using radiolabeled biomolecules is a translational molecular imaging technology that is increasingly used in support of drug development. Current methods for radiolabeling biomolecules with fluorine-18 are laborious and require multistep procedures with moderate labeling yields. The Al
    MeSH term(s) Aluminum Compounds/administration & dosage ; Animals ; Biological Factors/metabolism ; Chelating Agents/metabolism ; Fluorides/administration & dosage ; Fluorine Radioisotopes/administration & dosage ; Isotope Labeling/methods ; Macaca mulatta ; Positron-Emission Tomography/methods ; Temperature
    Chemical Substances Aluminum Compounds ; Biological Factors ; Chelating Agents ; Fluorine Radioisotopes ; Fluorine-18 (GZ5I74KB8G) ; Fluorides (Q80VPU408O) ; aluminum fluoride (Z77H3IKW94)
    Language English
    Publishing date 2017-07-14
    Publishing country Australia
    Document type Journal Article
    ZDB-ID 2592097-2
    ISSN 1838-7640 ; 1838-7640
    ISSN (online) 1838-7640
    ISSN 1838-7640
    DOI 10.7150/thno.20094
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Folate-PEG-NOTA-Al

    Chen, Qingshou / Meng, Xiangjun / McQuade, Paul / Rubins, Daniel / Lin, Shu-An / Zeng, Zhizhen / Haley, Hyking / Miller, Patricia / González Trotter, Dinko / Low, Philip S

    Molecular pharmaceutics

    2017  Volume 14, Issue 12, Page(s) 4353–4361

    Abstract: The folate receptor (FR) has been established as a promising target for imaging and therapy of cancer (FR-α), inflammation, and autoimmune diseases (FR-β). Several folate based PET radiotracers have been reported in the literature, but ... ...

    Abstract The folate receptor (FR) has been established as a promising target for imaging and therapy of cancer (FR-α), inflammation, and autoimmune diseases (FR-β). Several folate based PET radiotracers have been reported in the literature, but an
    MeSH term(s) A549 Cells ; Aluminum Compounds/chemistry ; Aluminum Compounds/pharmacokinetics ; Animals ; Drug Evaluation, Preclinical ; Female ; Fluorides/chemistry ; Fluorides/pharmacokinetics ; Fluorine Radioisotopes/chemistry ; Fluorine Radioisotopes/pharmacokinetics ; Folate Receptors, GPI-Anchored/metabolism ; Folic Acid/analogs & derivatives ; Folic Acid/chemistry ; Folic Acid/pharmacokinetics ; Heterocyclic Compounds/chemistry ; Heterocyclic Compounds/pharmacokinetics ; Humans ; Isotope Labeling/methods ; KB Cells ; Mice ; Mice, Nude ; Neoplasms/diagnostic imaging ; Neoplasms/pathology ; Organotechnetium Compounds ; Polyethylene Glycols/chemistry ; Polyethylene Glycols/pharmacokinetics ; Positron-Emission Tomography/methods ; Radiopharmaceuticals/chemistry ; Radiopharmaceuticals/pharmacokinetics ; Tissue Distribution ; X-Ray Microtomography/methods ; Xenograft Model Antitumor Assays
    Chemical Substances Aluminum Compounds ; Fluorine Radioisotopes ; Folate Receptors, GPI-Anchored ; Heterocyclic Compounds ; Organotechnetium Compounds ; Radiopharmaceuticals ; poly(ethylene glycol)-folate ; technetium 99m EC20 folate peptide ; Polyethylene Glycols (3WJQ0SDW1A) ; 1,4,7-triazacyclononane-N,N',N''-triacetic acid (56491-86-2) ; Folic Acid (935E97BOY8) ; Fluorine-18 (GZ5I74KB8G) ; Fluorides (Q80VPU408O) ; aluminum fluoride (Z77H3IKW94)
    Language English
    Publishing date 2017-11-01
    Publishing country United States
    Document type Comparative Study ; Journal Article
    ZDB-ID 2138405-8
    ISSN 1543-8392 ; 1543-8384
    ISSN (online) 1543-8392
    ISSN 1543-8384
    DOI 10.1021/acs.molpharmaceut.7b00415
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: A novel method for strict intranasal delivery of non-replicating RSV vaccines in cotton rats and non-human primates.

    Citron, Michael P / Patel, Manishkumar / Purcell, Mona / Lin, Shu-An / Rubins, Daniel J / McQuade, Paul / Callahan, Cheryl / Gleason, Alexa / Petrescu, Ioan / Knapp, Walter / Orekie, Chinedu / Chamarthy, Sai / Wen, Zhiyun / Touch, Sinoeun / Pine, Matthew / Fontenot, Jane / Douglas, Cameron / Liang, Xiaoping / Espeseth, Amy S

    Vaccine

    2018  Volume 36, Issue 20, Page(s) 2876–2885

    Abstract: Respiratory syncytial virus (RSV) is the most common viral cause of bronchiolitis and pneumonia in children twelve months of age or younger and a significant cause of lower respiratory disease in older adults. As various clinical and preclinical ... ...

    Abstract Respiratory syncytial virus (RSV) is the most common viral cause of bronchiolitis and pneumonia in children twelve months of age or younger and a significant cause of lower respiratory disease in older adults. As various clinical and preclinical candidates advance, cotton rats (Sigmodon hispidus) and non-human primates (NHP) continue to play a valuable role in RSV vaccine development, since both animals are semi-permissive to human RSV (HRSV). However, appropriate utilization of the models is critical to avoid mis-interpretation of the preclinical findings. Using a multimodality imaging approach; a fluorescence based optical imaging technique for the cotton rat and a nuclear medicine based positron emission tomography (PET) imaging technique for monkeys, we demonstrate that many common practices for intranasal immunization in both species result in inoculum delivery to the lower respiratory tract, which can result in poor translation of outcomes from the preclinical to the clinical setting. Using these technologies we define a method to limit the distribution of intranasally administered vaccines solely to the upper airway of each species, which includes volume restrictions in combination with injectable anesthesia. We show using our newly defined methods for strict intranasal immunization that these methods impact the immune responses and efficacy observed when compared to vaccination methods resulting in distribution to both the upper and lower respiratory tracts. These data emphasize the importance of well-characterized immunization methods in the preclinical assessment of intranasally delivered vaccine candidates.
    MeSH term(s) Administration, Intranasal ; Animals ; Cercopithecus aethiops ; Drug Evaluation, Preclinical/methods ; Female ; Models, Animal ; Respiratory Syncytial Virus Infections/prevention & control ; Respiratory Syncytial Virus Vaccines/administration & dosage ; Respiratory Syncytial Virus Vaccines/immunology ; Respiratory Syncytial Virus, Human/immunology ; Sigmodontinae
    Chemical Substances Respiratory Syncytial Virus Vaccines
    Language English
    Publishing date 2018-03-26
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 605674-x
    ISSN 1873-2518 ; 0264-410X
    ISSN (online) 1873-2518
    ISSN 0264-410X
    DOI 10.1016/j.vaccine.2018.02.110
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article ; Online: Synthesis and Preclinical Evaluation of Folate-NOTA-Al(18)F for PET Imaging of Folate-Receptor-Positive Tumors.

    Chen, Qingshou / Meng, Xiangjun / McQuade, Paul / Rubins, Daniel / Lin, Shu-An / Zeng, Zhizhen / Haley, Hyking / Miller, Patricia / González Trotter, Dinko / Low, Philip S

    Molecular pharmaceutics

    2016  Volume 13, Issue 5, Page(s) 1520–1527

    Abstract: Unlabelled: Folate-receptor-targeted PET radiotracers can potentially serve as versatile imaging agents for the diagnosis, staging, and prediction of response to therapy of patients with folate-receptor (FR)-expressing cancers. Because current FR- ... ...

    Abstract Unlabelled: Folate-receptor-targeted PET radiotracers can potentially serve as versatile imaging agents for the diagnosis, staging, and prediction of response to therapy of patients with folate-receptor (FR)-expressing cancers. Because current FR-targeted PET reagents can be compromised by complex labeling procedures, low specific activities, poor radiochemical yields, or unwanted accumulation in FR negative tissues, we have undertaken to design an improved folate-PET agent that might be more amenable for clinical development. For this purpose, we have synthesized a folate-NOTA-Al(18)F radiotracer and examined its properties both in vitro and in vivo.
    Methods: Radiochemical synthesis of folate-NOTA-Al(18)F was achieved by incubating (18)F(-) with AlCl3 for 2 min followed by heating in the presence of folate-NOTA for 15 min at 100 °C. Binding of folate-NOTA-Al(18)F to FR was quantitated in homogenates of KB and Cal51 tumor xenografts in the presence and absence of excess folic acid as a competitor. In vivo imaging was performed on nu/nu mice bearing either FR+ve (KB cell) or FR-ve (A549 cell) tumor xenografts, and specific accumulation of the radiotracer in tumor and other tissues was assessed by high-resolution micro-PET and ex vivo biodistribution in the presence and absence of excess folic acid. Image quality of folate-NOTA-Al(18)F was compared with that of (99m)Tc-EC20, a clinically established folate-targeted SPECT imaging agent.
    Results: Total radiochemical synthesis and purification of folate-NOTA-Al(18)F was completed within 37 min, yielding a specific activity of 68.82 ± 18.5 GBq/μmol, radiochemical yield of 18.6 ± 4.5%, and radiochemical purity of 98.3 ± 2.9%. Analysis of FR binding revealed a Kd of ∼1.0 nM, and micro-PET imaging together with ex vivo biodistribution analyses demonstrated high FR-mediated uptake in an FR+ tumor and the kidneys.
    Conclusions: Folate-NOTA-Al(18)F constitutes an easily prepared FR-targeted PET imaging agent with improved radiopharmaceutical properties and high specificity for folate receptor expressing tumors. Given its improved properties over (99m)Tc-EC20 (i.e., higher resolution, shorter image acquisition time, etc.), we conclude that folate-NOTA-Al(18)F constitutes a viable alternative to (99m)Tc-EC20 for use in identification, diagnosis, and staging of patients with FR-expressing cancers.
    MeSH term(s) A549 Cells ; Animals ; Female ; Fluorine Radioisotopes/chemistry ; Folate Receptors, GPI-Anchored/metabolism ; Folic Acid/administration & dosage ; Folic Acid/chemistry ; Heterocyclic Compounds/chemistry ; Humans ; KB Cells ; Mice ; Mice, Nude ; Neoplasms/diagnosis ; Neoplasms/metabolism ; Positron-Emission Tomography/methods ; Radiochemistry/methods ; Radiopharmaceuticals/chemistry ; Tissue Distribution ; Tomography, Emission-Computed, Single-Photon/methods
    Chemical Substances Fluorine Radioisotopes ; Folate Receptors, GPI-Anchored ; Heterocyclic Compounds ; Radiopharmaceuticals ; 1,4,7-triazacyclononane-N,N',N''-triacetic acid (56491-86-2) ; Folic Acid (935E97BOY8)
    Language English
    Publishing date 2016-05-02
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2138405-8
    ISSN 1543-8392 ; 1543-8384
    ISSN (online) 1543-8392
    ISSN 1543-8384
    DOI 10.1021/acs.molpharmaceut.5b00989
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  8. Article: Quantitative imaging with the micro-PET small-animal PET tomograph.

    Vaska, Paul / Rubins, Daniel J / Alexoff, David L / Schiffer, Wynne K

    International review of neurobiology

    2006  Volume 73, Page(s) 191–218

    MeSH term(s) Animals ; Animals, Laboratory/anatomy & histology ; Humans ; Image Interpretation, Computer-Assisted/methods ; Positron-Emission Tomography
    Language English
    Publishing date 2006
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 209876-3
    ISSN 0074-7742
    ISSN 0074-7742
    DOI 10.1016/S0074-7742(06)73006-9
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article: A novel method for strict intranasal delivery of non-replicating RSV vaccines in cotton rats and non-human primates

    Citron, Michael P / Callahan, Cheryl / Chamarthy, Sai / Douglas, Cameron / Espeseth, Amy S / Fontenot, Jane / Gleason, Alexa / Knapp, Walter / Liang, Xiaoping / Lin, Shu-An / McQuade, Paul / Orekie, Chinedu / Patel, Manishkumar / Petrescu, Ioan / Pine, Matthew / Purcell, Mona / Rubins, Daniel J / Touch, Sinoeun / Wen, Zhiyun

    Vaccine. 2018 May 11, v. 36, no. 20

    2018  

    Abstract: Respiratory syncytial virus (RSV) is the most common viral cause of bronchiolitis and pneumonia in children twelve months of age or younger and a significant cause of lower respiratory disease in older adults. As various clinical and preclinical ... ...

    Abstract Respiratory syncytial virus (RSV) is the most common viral cause of bronchiolitis and pneumonia in children twelve months of age or younger and a significant cause of lower respiratory disease in older adults. As various clinical and preclinical candidates advance, cotton rats (Sigmodon hispidus) and non-human primates (NHP) continue to play a valuable role in RSV vaccine development, since both animals are semi-permissive to human RSV (HRSV). However, appropriate utilization of the models is critical to avoid mis-interpretation of the preclinical findings. Using a multimodality imaging approach; a fluorescence based optical imaging technique for the cotton rat and a nuclear medicine based positron emission tomography (PET) imaging technique for monkeys, we demonstrate that many common practices for intranasal immunization in both species result in inoculum delivery to the lower respiratory tract, which can result in poor translation of outcomes from the preclinical to the clinical setting. Using these technologies we define a method to limit the distribution of intranasally administered vaccines solely to the upper airway of each species, which includes volume restrictions in combination with injectable anesthesia. We show using our newly defined methods for strict intranasal immunization that these methods impact the immune responses and efficacy observed when compared to vaccination methods resulting in distribution to both the upper and lower respiratory tracts. These data emphasize the importance of well-characterized immunization methods in the preclinical assessment of intranasally delivered vaccine candidates.
    Keywords anesthesia ; bronchiolitis ; children ; elderly ; fluorescence ; humans ; image analysis ; immune response ; inoculum ; medicine ; models ; monkeys ; pneumonia ; positron-emission tomography ; Primates ; Respiratory syncytial virus ; respiratory system ; Sigmodon hispidus ; vaccination ; vaccine development ; vaccines
    Language English
    Dates of publication 2018-0511
    Size p. 2876-2885.
    Publishing place Elsevier Ltd
    Document type Article
    ZDB-ID 605674-x
    ISSN 1873-2518 ; 0264-410X
    ISSN (online) 1873-2518
    ISSN 0264-410X
    DOI 10.1016/j.vaccine.2018.02.110
    Database NAL-Catalogue (AGRICOLA)

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  10. Article ; Online: MK-8719, a Novel and Selective

    Wang, Xiaohai / Li, Wenping / Marcus, Jacob / Pearson, Michelle / Song, Lixin / Smith, Karen / Terracina, Giuseppe / Lee, Julie / Hong, Kwok-Lam Karen / Lu, Sherry X / Hyde, Lynn / Chen, Shu-Cheng / Kinsley, David / Melchor, Jerry P / Rubins, Daniel J / Meng, Xiangjun / Hostetler, Eric / Sur, Cyrille / Zhang, Lili /
    Schachter, Joel B / Hess, J Fred / Selnick, Harold G / Vocadlo, David J / McEachern, Ernest J / Uslaner, Jason M / Duffy, Joseph L / Smith, Sean M

    The Journal of pharmacology and experimental therapeutics

    2020  Volume 374, Issue 2, Page(s) 252–263

    Abstract: Deposition of hyperphosphorylated and aggregated tau protein in the central nervous system is characteristic of Alzheimer disease and other tauopathies. Tau is subject ... ...

    Abstract Deposition of hyperphosphorylated and aggregated tau protein in the central nervous system is characteristic of Alzheimer disease and other tauopathies. Tau is subject to
    MeSH term(s) Animals ; Atrophy/drug therapy ; Brain/drug effects ; Brain/metabolism ; Brain/pathology ; Disease Models, Animal ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/therapeutic use ; Locomotion/drug effects ; Male ; Mice ; PC12 Cells ; Rats ; Tauopathies/drug therapy ; Tauopathies/metabolism ; Tauopathies/pathology ; Tauopathies/physiopathology ; beta-N-Acetylhexosaminidases/antagonists & inhibitors ; tau Proteins/metabolism
    Chemical Substances Enzyme Inhibitors ; tau Proteins ; hexosaminidase C (EC 3.2.1.50) ; beta-N-Acetylhexosaminidases (EC 3.2.1.52)
    Language English
    Publishing date 2020-06-03
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 3106-9
    ISSN 1521-0103 ; 0022-3565
    ISSN (online) 1521-0103
    ISSN 0022-3565
    DOI 10.1124/jpet.120.266122
    Database MEDical Literature Analysis and Retrieval System OnLINE

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