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  1. Article ; Online: Investigation of the terminal P4 domain in a series of D-phenylglycinamide-based factor Xa inhibitors.

    Franciskovich, Jeffry B / Masters, John J / Weber, Wayne W / Klimkowski, Valentine J / Chouinard, Michael / Sipes, Philip R / Johnson, Lea M / Snyder, David W / Chastain, Marcia K / Craft, Trelia J / Towner, Richard D / Gifford-Moore, Donetta S / Froelich, Larry L / Smallwood, Jeffrey K / Foster, Ronald S / Smith, Gerald F / Liebeschuetz, John W / Murray, Christopher W / Young, Stephen C

    Bioorganic & medicinal chemistry letters

    2007  Volume 17, Issue 24, Page(s) 6910–6913

    Abstract: ... synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent ... Several P4 domain derivatives of the general d-phenylglycinamide-based scaffold (2) were ...

    Abstract Several P4 domain derivatives of the general d-phenylglycinamide-based scaffold (2) were synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent compounds were evaluated for their anticoagulant effects in vitro. A select subset containing various P1 indole constructs was further evaluated for their pharmacokinetic properties after oral administration to rats.
    MeSH term(s) Anticoagulants/chemical synthesis ; Anticoagulants/chemistry ; Anticoagulants/pharmacology ; Antithrombin III/chemical synthesis ; Antithrombin III/chemistry ; Antithrombin III/pharmacology ; Crystallography, X-Ray ; Factor Xa/chemistry ; Factor Xa/metabolism ; Glycine/analogs & derivatives ; Glycine/chemical synthesis ; Glycine/chemistry ; Glycine/pharmacology ; Humans ; Models, Molecular ; Molecular Structure ; Protein Binding ; Structure-Activity Relationship
    Chemical Substances Anticoagulants ; phenylglycinamide ; Antithrombin III (9000-94-6) ; Factor Xa (EC 3.4.21.6) ; Glycine (TE7660XO1C)
    Language English
    Publishing date 2007-12-15
    Publishing country England
    Document type Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2007.09.105
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Acute renal syndrome/renal angina: a new paradigm for studies of acute kidney injury?

    Johnson, Xa D / Liu, Kathleen D

    Clinical journal of the American Society of Nephrology : CJASN

    2010  Volume 5, Issue 5, Page(s) 753–755

    MeSH term(s) Acute Disease ; Biomarkers/blood ; Critical Care ; Early Diagnosis ; Health Status Indicators ; Humans ; Kidney/metabolism ; Kidney Diseases/blood ; Kidney Diseases/diagnosis ; Kidney Diseases/etiology ; Kidney Diseases/mortality ; Kidney Diseases/therapy ; Predictive Value of Tests ; Risk Assessment ; Risk Factors ; Syndrome ; Terminology as Topic
    Chemical Substances Biomarkers
    Language English
    Publishing date 2010-05
    Publishing country United States
    Document type Comment ; Editorial
    ZDB-ID 2226665-3
    ISSN 1555-905X ; 1555-9041
    ISSN (online) 1555-905X
    ISSN 1555-9041
    DOI 10.2215/CJN.02360310
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Effect of plasma-activated water and buffer solution combined with ultrasound on fungicide degradation and quality of cherry tomato during storage.

    Ali, Murtaza / Cheng, Jun-Hu / Tazeddinova, Diana / Aadil, Rana Muhammad / Zeng, Xin-An / Goksen, Gulden / Lorenzo, Jose Manuel / Esua, Okon Johnson / Manzoor, Muhammad Faisal

    Ultrasonics sonochemistry

    2023  Volume 97, Page(s) 106461

    Abstract: The purpose of this study was to examine plasma-activated buffer solution (PABS) and plasma-activated water (PAW) combined with ultrasonication (U) treatment on the reduction of chlorothalonil fungicide and the quality of tomato fruits during storage. To ...

    Abstract The purpose of this study was to examine plasma-activated buffer solution (PABS) and plasma-activated water (PAW) combined with ultrasonication (U) treatment on the reduction of chlorothalonil fungicide and the quality of tomato fruits during storage. To obtain PAW and PABS, an atmospheric air plasma jet was used to treat buffer solution and deionized water at different treatment times (5 and 10 min). For combined treatments, fruits were submerged in PAW and PABS, then sonicated for 15 min, and individual treatment without sonication. As per the results, the maximum chlorothalonil reduction of 89.29% was detected in PAW-U
    MeSH term(s) Water/chemistry ; Fungicides, Industrial ; Solanum lycopersicum ; Nitriles
    Chemical Substances Water (059QF0KO0R) ; tetrachloroisophthalonitrile (J718M71A7A) ; Fungicides, Industrial ; Nitriles
    Language English
    Publishing date 2023-05-30
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 1208333-1
    ISSN 1873-2828 ; 1350-4177
    ISSN (online) 1873-2828
    ISSN 1350-4177
    DOI 10.1016/j.ultsonch.2023.106461
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: SLC25A51 is a mammalian mitochondrial NAD

    Luongo, Timothy S / Eller, Jared M / Lu, Mu-Jie / Niere, Marc / Raith, Fabio / Perry, Caroline / Bornstein, Marc R / Oliphint, Paul / Wang, Lin / McReynolds, Melanie R / Migaud, Marie E / Rabinowitz, Joshua D / Johnson, F Brad / Johnsson, Kai / Ziegler, Mathias / Cambronne, Xiaolu A / Baur, Joseph A

    Nature

    2020  Volume 588, Issue 7836, Page(s) 174–179

    Abstract: Mitochondria require nicotinamide adenine dinucleotide ( ... ...

    Abstract Mitochondria require nicotinamide adenine dinucleotide (NAD
    MeSH term(s) Animals ; Biological Transport ; Cell Line ; Cell Respiration/genetics ; Genetic Complementation Test ; Humans ; Mice ; Mitochondria/genetics ; Mitochondria/metabolism ; Mitochondria/pathology ; Mitochondrial Proteins/deficiency ; Mitochondrial Proteins/genetics ; Mitochondrial Proteins/metabolism ; NAD/metabolism ; Nucleotide Transport Proteins/genetics ; Organic Cation Transport Proteins/deficiency ; Organic Cation Transport Proteins/genetics ; Saccharomyces cerevisiae/cytology ; Saccharomyces cerevisiae/genetics ; Saccharomyces cerevisiae/metabolism ; Saccharomyces cerevisiae Proteins/genetics
    Chemical Substances Mitochondrial Proteins ; Ndt1 protein, S cerevisiae ; Nucleotide Transport Proteins ; Organic Cation Transport Proteins ; Saccharomyces cerevisiae Proteins ; NAD (0U46U6E8UK)
    Language English
    Publishing date 2020-09-09
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 120714-3
    ISSN 1476-4687 ; 0028-0836
    ISSN (online) 1476-4687
    ISSN 0028-0836
    DOI 10.1038/s41586-020-2741-7
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: The use of betrixaban for extended prophylaxis of venous thromboembolism events in hospitalized, high-risk patients.

    Dobesh, Paul P / Ahuja, Tania / Davis, George A / Fatodu, Hugh / Francis, William H / Hull, Frank P / Johnson, Gary L / Lenchus, Joshua D / Lenoir, Jacqueline Glee / McPherson, Claudette / Nemeth, Jeffrey / Riello, Ralph J

    The American journal of managed care

    2018  Volume 24, Issue 22 Suppl, Page(s) S475–S482

    MeSH term(s) Acute Disease ; Aged ; Benzamides/administration & dosage ; Benzamides/therapeutic use ; Factor Xa Inhibitors/administration & dosage ; Factor Xa Inhibitors/therapeutic use ; Female ; Health Care Costs ; Hospitalization ; Humans ; Male ; Primary Prevention ; Pyridines/administration & dosage ; Pyridines/therapeutic use ; Randomized Controlled Trials as Topic ; Risk Factors ; United States/epidemiology ; Venous Thromboembolism/epidemiology ; Venous Thromboembolism/prevention & control
    Chemical Substances Benzamides ; Factor Xa Inhibitors ; Pyridines ; betrixaban (74RWP7W0J9)
    Language English
    Publishing date 2018-11-19
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2035781-3
    ISSN 1936-2692 ; 1088-0224 ; 1096-1860
    ISSN (online) 1936-2692
    ISSN 1088-0224 ; 1096-1860
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Oral anticoagulation is preferable to injected, but only if it is safe and effective: An interview study of patient and carer experience of oral and injected anticoagulant therapy for cancer-associated thrombosis in the select-d trial.

    Hutchinson, Ann / Rees, Sophie / Young, Annie / Maraveyas, Anthony / Date, Kathryn / Johnson, Miriam J

    Palliative medicine

    2018  Volume 33, Issue 5, Page(s) 510–517

    Abstract: ... benefit of thrombosis treatment.: Design: Qualitative substudy of the select-d trial, using semi ... of low-molecular-weight heparin. The 'select-d' trial is an open-label, randomised, multi-centre pilot trial in patients ...

    Abstract Background: Cancer patients have a four- to fivefold greater risk of thrombosis than the general population. Recommended treatment for cancer-associated thrombosis is 3-6 months of low-molecular-weight heparin. The 'select-d' trial is an open-label, randomised, multi-centre pilot trial in patients with cancer-associated thrombosis, utilising dalteparin (low-molecular-weight heparin) versus rivaroxaban (a direct oral anticoagulant), to assess effectiveness and safety.
    Aim: To explore patient and informal carers' experiences of cancer-associated thrombosis and their experience and understanding of the risk-benefit of thrombosis treatment.
    Design: Qualitative substudy of the select-d trial, using semi-structured interviews. Interviews were audio-recorded and transcribed. Data were analysed using Framework Analysis.
    Participants: Participants were purposively sampled ( n = 37 patients; 46% male; age 40-89; 9 with carer present).
    Results: Three themes were found: experience of cancer-associated thrombosis, experience of anticoagulation and risk-benefit balance of the two modes of administration. Some were shocked by their thrombosis diagnosis (most were unaware of their risk), but others found it insignificant compared with cancer. Most patients found tablets more convenient, but injections were acceptable in the context of having cancer. While most were happy to follow medical advice, others weighed preference on the basis of effectiveness.
    Conclusion: Lack of awareness of thrombosis risk is concerning; cancer patients must be informed to enable prompt help-seeking. Tablets could provide a welcome choice for patients if there is equivalent risk-benefit to injected anticoagulants. Patients trust their clinicians to tailor their treatment. Future research could explore the effect of routine information giving about the risk of thrombosis.
    MeSH term(s) Administration, Oral ; Adult ; Aged ; Aged, 80 and over ; Anticoagulants/administration & dosage ; Dalteparin/administration & dosage ; Factor Xa Inhibitors/administration & dosage ; Female ; Humans ; Injections ; Male ; Middle Aged ; Neoplasms/complications ; Patient Satisfaction ; Rivaroxaban/administration & dosage ; Venous Thrombosis/prevention & control
    Chemical Substances Anticoagulants ; Factor Xa Inhibitors ; Rivaroxaban (9NDF7JZ4M3) ; Dalteparin (S79O08V79F)
    Language English
    Publishing date 2018-11-29
    Publishing country England
    Document type Journal Article ; Multicenter Study ; Randomized Controlled Trial ; Research Support, Non-U.S. Gov't
    ZDB-ID 639247-7
    ISSN 1477-030X ; 0269-2163
    ISSN (online) 1477-030X
    ISSN 0269-2163
    DOI 10.1177/0269216318815377
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  7. Article ; Online: Best practices for implementing venous thromboembolism prophylaxis across the continuum of care.

    Dobesh, Paul P / Ahuja, Tania / Davis, George A / Fatodu, Hugh / Francis, William H / Hull, Frank P / Johnson, Gary L / Lenchus, Joshua D / Lenoir, Jacqueline Glee / McPherson, Claudette / Nemeth, Jeffrey / Riello, Ralph J

    The American journal of managed care

    2018  Volume 24, Issue 22 Suppl, Page(s) S483–S488

    MeSH term(s) Anticoagulants/therapeutic use ; Benzamides/therapeutic use ; Factor Xa Inhibitors/therapeutic use ; Hospitalization ; Humans ; Primary Prevention ; Pyridines/therapeutic use ; Risk Assessment/methods ; Risk Factors ; Transitional Care/standards ; United States ; Venous Thromboembolism/prevention & control
    Chemical Substances Anticoagulants ; Benzamides ; Factor Xa Inhibitors ; Pyridines ; betrixaban (74RWP7W0J9)
    Language English
    Publishing date 2018-11-19
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2035781-3
    ISSN 1936-2692 ; 1088-0224 ; 1096-1860
    ISSN (online) 1936-2692
    ISSN 1088-0224 ; 1096-1860
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  8. Article ; Online: Synthesis, Binding Mode, and Antihyperglycemic Activity of Potent and Selective (5-Imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine Inhibitors of Glycogen Synthase Kinase 3.

    Wagman, Allan S / Boyce, Rustum S / Brown, Sean P / Fang, Eric / Goff, Dane / Jansen, Johanna M / Le, Vincent P / Levine, Barry H / Ng, Simon C / Ni, Zhi-Jie / Nuss, John M / Pfister, Keith B / Ramurthy, Savithri / Renhowe, Paul A / Ring, David B / Shu, Wei / Subramanian, Sharadha / Zhou, Xiaohui A / Shafer, Cynthia M /
    Harrison, Stephen D / Johnson, Kirk W / Bussiere, Dirksen E

    Journal of medicinal chemistry

    2017  Volume 60, Issue 20, Page(s) 8482–8514

    Abstract: In an effort to identify new antidiabetic agents, we have discovered a novel family of (5-imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine analogues which are inhibitors of human glycogen synthase kinase 3 (GSK3). We developed ... ...

    Abstract In an effort to identify new antidiabetic agents, we have discovered a novel family of (5-imidazol-2-yl-4-phenylpyrimidin-2-yl)[2-(2-pyridylamino)ethyl]amine analogues which are inhibitors of human glycogen synthase kinase 3 (GSK3). We developed efficient synthetic routes to explore a wide variety of substitution patterns and convergently access a diverse array of analogues. Compound 1 (CHIR-911, CT-99021, or CHIR-73911) emerged from an exploration of heterocycles at the C-5 position, phenyl groups at C-4, and a variety of differently substituted linker and aminopyridine moieties attached at the C-2 position. These compounds exhibited GSK3 IC
    MeSH term(s) Animals ; CHO Cells ; Chromatography, High Pressure Liquid ; Cricetulus ; Crystallography, X-Ray ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/pharmacology ; Glycogen Synthase Kinases/antagonists & inhibitors ; Humans ; Hypoglycemic Agents/chemical synthesis ; Hypoglycemic Agents/metabolism ; Hypoglycemic Agents/pharmacology ; Mass Spectrometry ; Proton Magnetic Resonance Spectroscopy ; Pyrimidines/chemistry ; Pyrimidines/metabolism ; Pyrimidines/pharmacology ; Rats ; Structure-Activity Relationship
    Chemical Substances Enzyme Inhibitors ; Hypoglycemic Agents ; Pyrimidines ; Glycogen Synthase Kinases (EC 2.7.11.-)
    Language English
    Publishing date 2017-10-10
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.7b00922
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  9. Article ; Online: Crystal structure of the prothrombinase complex from the venom of Pseudonaja textilis.

    Lechtenberg, Bernhard C / Murray-Rust, Thomas A / Johnson, Daniel J D / Adams, Ty E / Krishnaswamy, Sriram / Camire, Rodney M / Huntington, James A

    Blood

    2013  Volume 122, Issue 16, Page(s) 2777–2783

    Abstract: The prothrombinase complex, composed of the protease factor (f)Xa and cofactor fVa, efficiently ...

    Abstract The prothrombinase complex, composed of the protease factor (f)Xa and cofactor fVa, efficiently converts prothrombin to thrombin by specific sequential cleavage at 2 sites. How the complex assembles and its mechanism of prothrombin processing are of central importance to human health and disease, because insufficient thrombin generation is the root cause of hemophilia, and excessive thrombin production results in thrombosis. Efforts to determine the crystal structure of the prothrombinase complex have been thwarted by the dependence of complex formation on phospholipid membrane association. Pseutarin C is an intrinsically stable prothrombinase complex preassembled in the venom gland of the Australian Eastern Brown Snake (Pseudonaja textilis). Here we report the crystal structures of the fX-fV complex and of activated fXa from P textilis venom and the derived model of active pseutarin C. Structural analysis supports a single substrate binding channel on fVa, to which prothrombin and the intermediate meizothrombin bind in 2 different orientations, providing insight into the architecture and mechanism of the prothrombinase complex-the molecular engine of blood coagulation.
    MeSH term(s) Animals ; Binding Sites ; Blood Coagulation ; Crystallography, X-Ray ; Elapid Venoms/chemistry ; Factor V/chemistry ; Factor Xa/chemistry ; Humans ; Models, Molecular ; Mutation ; Protein Conformation ; Protein Structure, Tertiary ; Snake Venoms/enzymology ; Snakes ; Thromboplastin/chemistry
    Chemical Substances Elapid Venoms ; Pseutarin C ; Snake Venoms ; prothrombinase complex ; Factor V (9001-24-5) ; Thromboplastin (9035-58-9) ; Factor Xa (EC 3.4.21.6)
    Language English
    Publishing date 2013-07-18
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 80069-7
    ISSN 1528-0020 ; 0006-4971
    ISSN (online) 1528-0020
    ISSN 0006-4971
    DOI 10.1182/blood-2013-06-511733
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article: Antithrombin-S195A factor Xa-heparin structure reveals the allosteric mechanism of antithrombin activation.

    Johnson, Daniel J D / Li, Wei / Adams, Ty E / Huntington, James A

    The EMBO journal

    2006  Volume 25, Issue 9, Page(s) 2029–2037

    Abstract: ... IXa and Xa. Here we present the crystallographic structure of the recognition (Michaelis) complex ...

    Abstract Regulation of blood coagulation is critical for maintaining blood flow, while preventing excessive bleeding or thrombosis. One of the principal regulatory mechanisms involves heparin activation of the serpin antithrombin (AT). Inhibition of several coagulation proteases is accelerated by up to 10,000-fold by heparin, either through bridging AT and the protease or by inducing allosteric changes in the properties of AT. The anticoagulant effect of short heparin chains, including the minimal AT-specific pentasaccharide, is mediated exclusively through the allosteric activation of AT towards efficient inhibition of coagulation factors (f) IXa and Xa. Here we present the crystallographic structure of the recognition (Michaelis) complex between heparin-activated AT and S195A fXa, revealing the extensive exosite contacts that confer specificity. The heparin-induced conformational change in AT is required to allow simultaneous contacts within the active site and two distinct exosites of fXa (36-loop and the autolysis loop). This structure explains the molecular basis of protease recognition by AT, and the mechanism of action of the important therapeutic low-molecular-weight heparins.
    MeSH term(s) Allosteric Regulation ; Animals ; Antithrombin III/antagonists & inhibitors ; Antithrombin III/chemistry ; Crystallography ; Factor Xa/chemistry ; Factor Xa/genetics ; Fibrinolytic Agents/chemistry ; Fibrinolytic Agents/pharmacology ; Heparin/chemistry ; Heparin/pharmacology ; Humans ; Protein Conformation
    Chemical Substances Fibrinolytic Agents ; Antithrombin III (9000-94-6) ; Heparin (9005-49-6) ; Factor Xa (EC 3.4.21.6)
    Language English
    Publishing date 2006-04-13
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 586044-1
    ISSN 1460-2075 ; 0261-4189
    ISSN (online) 1460-2075
    ISSN 0261-4189
    DOI 10.1038/sj.emboj.7601089
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