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  1. Article ; Online: GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A

    Shiriaeva, Anna / Park, Daejin / Kim, Gyudong / Lee, Yoonji / Hou, Xiyan / Jarhad, Dnyandev B / Kim, Gibae / Yu, Jinha / Hyun, Young Eum / Kim, Woomi / Gao, Zhan-Guo / Jacobson, Kenneth A / Han, Gye Won / Stevens, Raymond C / Jeong, Lak Shin / Choi, Sun / Cherezov, Vadim

    Journal of medicinal chemistry

    2022  Volume 65, Issue 17, Page(s) 11648–11657

    Abstract: Modulators of the G protein-coupled ... ...

    Abstract Modulators of the G protein-coupled A
    MeSH term(s) Adenosine A2 Receptor Antagonists/chemistry ; Adenosine A2 Receptor Antagonists/pharmacology ; Crystallography, X-Ray ; Molecular Conformation ; Nucleosides ; Receptor, Adenosine A2A/chemistry ; Thiophenes
    Chemical Substances Adenosine A2 Receptor Antagonists ; Nucleosides ; Receptor, Adenosine A2A ; Thiophenes
    Language English
    Publishing date 2022-08-17
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S. ; Research Support, N.I.H., Intramural
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.2c00462
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Bioequivalence of a single 400-mg dose of imatinib 100-mg oral tablets and a 400-mg tablet in healthy adult Korean volunteers.

    Lee, Hae Won / Seong, Sook Jin / Park, Sung Min / Lee, Joomi / Gwon, Mi-Ri / Kim, Hyun-Ju / Lim, Sung Mook / Lim, Mi-Sun / Kim, Woomi / Yang, Dong Heon / Yoon, Young-Ran

    International journal of clinical pharmacology and therapeutics

    2015  Volume 53, Issue 6, Page(s) 480–487

    Abstract: Background: Imatinib mesylate (IM) is a selective tyrosine kinase inhibitor for the treatment of chronic myeloid leukemia and gastrointestinal stromal tumors. A new once-daily 400-mg film-coated tablet of imatinib has been developed by a pharmaceutical ... ...

    Abstract Background: Imatinib mesylate (IM) is a selective tyrosine kinase inhibitor for the treatment of chronic myeloid leukemia and gastrointestinal stromal tumors. A new once-daily 400-mg film-coated tablet of imatinib has been developed by a pharmaceutical company in Korea.
    Objective: The present study was designed to assess and compare the PK parameters, bioavailability, and bioequivalence of the new imatinib 400-mg formulation (test) versus the conventional 100-mg formulation (reference) administered as a single 400-mg dose in healthy adult male volunteers.
    Methods: This randomized, open-label, single-dose, two-way crossover study was conducted in healthy Korean male volunteers. Eligible subjects were randomly assigned in a 1 : 1 ratio to receive 400 mg of the test (one 400-mg tablet) or reference (four 100-mg tablets) formulation, followed by a 2-week washout period and administration of the alternate formulation. Serial blood samples were collected at 0 (predose), 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24, 48, and 72 hours after administration. Plasma imatinib concentrations were determined using liquid chromatography coupled with tandem mass spectrometry. The formulations were to be considered bioequivalent if the 90% confidence intervals (CIs) of the adjusted geometric mean ratios for Cmax, AUC(0-t), and AUC(0-∞)ž were within the predetermined range of 0.80 - 1.25.
    Results: In total, 35 subjects completed the study. No serious adverse event was reported during the study. The 90% CIs of the adjusted geometric mean ratios of the test formulation to the reference formulation for C(max), AUC(0-t) and AUC(0-∞)ž of imatinib were all within the bioequivalence criteria range of 0.8 - 1.25.
    Conclusions: The test formulation of imatinib met the Korean regulatory requirements for bioequivalence. Both imatinib formulations were well-tolerated in all subjects.
    MeSH term(s) Administration, Oral ; Adult ; Antineoplastic Agents/administration & dosage ; Antineoplastic Agents/adverse effects ; Antineoplastic Agents/blood ; Antineoplastic Agents/pharmacokinetics ; Area Under Curve ; Asian Continental Ancestry Group ; Benzamides/administration & dosage ; Benzamides/adverse effects ; Benzamides/blood ; Benzamides/pharmacokinetics ; Biological Availability ; Chromatography, Liquid ; Cross-Over Studies ; Drug Monitoring ; Half-Life ; Healthy Volunteers ; Humans ; Imatinib Mesylate ; Male ; Metabolic Clearance Rate ; Middle Aged ; Piperazines/administration & dosage ; Piperazines/adverse effects ; Piperazines/blood ; Piperazines/pharmacokinetics ; Protein Kinase Inhibitors/administration & dosage ; Protein Kinase Inhibitors/adverse effects ; Protein Kinase Inhibitors/blood ; Protein Kinase Inhibitors/pharmacokinetics ; Pyrimidines/administration & dosage ; Pyrimidines/adverse effects ; Pyrimidines/blood ; Pyrimidines/pharmacokinetics ; Republic of Korea ; Tablets ; Tandem Mass Spectrometry ; Therapeutic Equivalency ; Young Adult
    Chemical Substances Antineoplastic Agents ; Benzamides ; Piperazines ; Protein Kinase Inhibitors ; Pyrimidines ; Tablets ; Imatinib Mesylate (8A1O1M485B)
    Language English
    Publishing date 2015-06
    Publishing country Germany
    Document type Comparative Study ; Journal Article ; Randomized Controlled Trial ; Research Support, Non-U.S. Gov't
    ZDB-ID 124384-6
    ISSN 0946-1965 ; 0340-0026 ; 0300-9718 ; 0174-4879
    ISSN 0946-1965 ; 0340-0026 ; 0300-9718 ; 0174-4879
    DOI 10.5414/CP202267
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 467: Show issues Location:
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  3. Article: An Improved UPLC Method for Rapid Analysis of Levofloxacin in Human Plasma

    Park, Dae-Jin / Phapale, Prasad B / Jang, In-Jin / Cui, Song / Moon, Byung-Jo / Kim, Jung-Eun / Kim, Woomi / Hwang, Sung-Kyu / Yoon, Young-Ran

    Chromatographia. 2008 Aug., v. 68, no. 3-4

    2008  

    Abstract: A rapid, specific, and sensitive ultra-performance liquid chromatographic method for analysis of levofloxacin in human plasma has been developed and validated. Plasma samples were spiked with the internal standard (enoxacin) and extracted with 10:1 (v/v) ...

    Abstract A rapid, specific, and sensitive ultra-performance liquid chromatographic method for analysis of levofloxacin in human plasma has been developed and validated. Plasma samples were spiked with the internal standard (enoxacin) and extracted with 10:1 (v/v) ethyl acetate-isopropanol. UPLC was performed on a 100 x 2.1 mm i.d., 1.7 μm particle, C₁₈ column with 88:12 (v/v) 0.4% triethylamine buffer (pH 3)-acetonitrile as mobile phase, pumped isocratically at a pressure of 11,000 psi (758 bar) and a flow-rate of 0.3 mL min⁻¹. Ultraviolet detection was performed at 300 nm. The retention times of levofloxacin and enoxacin were 3.4 and 2.8 min, respectively, and the run-time was 5 min. Calibration showed that response was a linear function of concentration over the range 0.05-10 μg mL⁻¹ (r ² >= 0.99) and the method was validated over this range for both precision and accuracy. The relative standard deviation was <15% for both intra-day and inter-day assay (n = 5). Levofloxacin and enoxacin were stable in plasma; there was no evidence of degradation during three freeze-thaw cycles, post-preparative stability at 20 °C was >=24 h, short-term stability at room temperature was >=6 h, and long-term stability at -70 °C was >=30 days. The method was successfully used in a study of the bioequivalence of two levofloxacin tablet formulations in healthy volunteers.
    Language English
    Dates of publication 2008-08
    Size p. 187-192.
    Publisher Vieweg Verlag
    Publishing place Wiesbaden
    Document type Article
    ZDB-ID 80097-1
    ISSN 0009-5893
    ISSN 0009-5893
    DOI 10.1365/s10337-008-0669-4
    Database NAL-Catalogue (AGRICOLA)

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    Zs.A 4557: Show issues Location:
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  4. Article: Trends in enzyme therapy for phenylketonuria.

    Kim, Woomi / Erlandsen, Heidi / Surendran, Sankar / Stevens, Raymond C / Gamez, Alejandra / Michols-Matalon, Kimberlee / Tyring, Stephen K / Matalon, Reuben

    Molecular therapy : the journal of the American Society of Gene Therapy

    2004  Volume 10, Issue 2, Page(s) 220–224

    Abstract: Phenylketonuria (PKU) is an inborn error of amino acid metabolism caused by phenylalanine hydroxylase (PAH) deficiency. Dietary treatment has been the cornerstone for controlling systemic phenylalanine (Phe) levels in PKU for the past 4 decades. Over the ...

    Abstract Phenylketonuria (PKU) is an inborn error of amino acid metabolism caused by phenylalanine hydroxylase (PAH) deficiency. Dietary treatment has been the cornerstone for controlling systemic phenylalanine (Phe) levels in PKU for the past 4 decades. Over the years, it has become clear that blood Phe concentration needs to be controlled for the life of the patient, a difficult task taking into consideration that the diet becomes very difficult to maintain. Therefore alternative models of therapy are being pursued. This review describes the progress made in enzyme replacement therapy for PKU. Two modalities are discussed, PAH and phenylalanine ammonia-lyase PAH. Developing stable and functional forms of both enzymes has proven difficult, but recent success in producing polyethylene glycol-modified forms of active and stable PAH shows promise.
    MeSH term(s) Biopterins/analogs & derivatives ; Biopterins/pharmacology ; Capsules/chemistry ; Drug Therapy/methods ; Drug Therapy/trends ; Humans ; Phenylalanine Ammonia-Lyase/chemistry ; Phenylalanine Ammonia-Lyase/metabolism ; Phenylalanine Ammonia-Lyase/therapeutic use ; Phenylalanine Hydroxylase/chemistry ; Phenylalanine Hydroxylase/metabolism ; Phenylalanine Hydroxylase/therapeutic use ; Phenylketonurias/drug therapy ; Phenylketonurias/metabolism ; Polyethylene Glycols/chemistry
    Chemical Substances Capsules ; Biopterins ; Polyethylene Glycols (3WJQ0SDW1A) ; Phenylalanine Hydroxylase (EC 1.14.16.1) ; Phenylalanine Ammonia-Lyase (EC 4.3.1.24) ; sapropterin (EGX657432I)
    Language English
    Publishing date 2004-08-04
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 2010592-7
    ISSN 1525-0024 ; 1525-0016
    ISSN (online) 1525-0024
    ISSN 1525-0016
    DOI 10.1016/j.ymthe.2004.05.001
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 5640: Show issues Location:
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  5. Article: Development of pegylated forms of recombinant Rhodosporidium toruloides phenylalanine ammonia-lyase for the treatment of classical phenylketonuria.

    Gámez, Alejandra / Sarkissian, Christineh N / Wang, Lin / Kim, Woomi / Straub, Mary / Patch, Marianne G / Chen, Lin / Striepeke, Steve / Fitzpatrick, Paul / Lemontt, Jeffrey F / O'Neill, Charles / Scriver, Charles R / Stevens, Raymond C

    Molecular therapy : the journal of the American Society of Gene Therapy

    2005  Volume 11, Issue 6, Page(s) 986–989

    Abstract: Phenylketonuria (PKU) is a metabolic disorder due primarily to mutations in the PAH gene that impair both phenylalanine hydroxylase activity and disposal of l-phenylalanine from the normal diet. Excess phenylalanine is toxic to cognitive development and ... ...

    Abstract Phenylketonuria (PKU) is a metabolic disorder due primarily to mutations in the PAH gene that impair both phenylalanine hydroxylase activity and disposal of l-phenylalanine from the normal diet. Excess phenylalanine is toxic to cognitive development and a low-phenylalanine diet prevents mental retardation, but it is a difficult therapeutic option. Previous studies with recombinant phenylalanine ammonia-lyase, PAL, demonstrated pharmacologic and physiologic proofs of principle for PAL as an alternative therapy for PKU but its immunogenicity was problematic. From a series of formulations of linear and branched polyethylene glycols chemically conjugated to PAL, we have created a parenteral therapeutic agent for PKU treatment. All the pegylated molecules were fully characterized in vitro and the most promising formulations were then tested in vivo in the PKU mouse model. The linear 20-kDa PEG-PAL combination abolished in vivo immunogenicity after repeated challenge while retaining full catabolic activity against phenylalanine, suggesting potential as a novel PKU therapeutic.
    MeSH term(s) Animals ; Antibodies/blood ; Humans ; Mice ; Phenylalanine Ammonia-Lyase/chemistry ; Phenylalanine Ammonia-Lyase/immunology ; Phenylalanine Ammonia-Lyase/therapeutic use ; Phenylketonurias/drug therapy ; Polyethylene Glycols/chemistry ; Polyethylene Glycols/therapeutic use ; Recombinant Proteins/chemistry ; Recombinant Proteins/immunology ; Recombinant Proteins/therapeutic use
    Chemical Substances Antibodies ; Recombinant Proteins ; Polyethylene Glycols (30IQX730WE) ; Phenylalanine Ammonia-Lyase (EC 4.3.1.24)
    Language English
    Publishing date 2005-06
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2010592-7
    ISSN 1525-0024 ; 1525-0016
    ISSN (online) 1525-0024
    ISSN 1525-0016
    DOI 10.1016/j.ymthe.2005.02.013
    Database MEDical Literature Analysis and Retrieval System OnLINE

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