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  1. Article ; Online: Prokinetic actions of luminally acting 5-HT

    Konen, John R / Haag, Melody M / Guseva, Daria / Hurd, Molly / Linton, Alisha A / Lavoie, Brigitte / Kerrigan, Colleen B / Joyce, Emily / Bischoff, Stephan C / Swann, Steve / Griffin, Luana / Matsukawa, Jun / Falk, Matthew D / Gibson, Tony S / Hennig, Grant W / Wykosky, Jill / Mawe, Gary M

    Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society

    2020  Volume 33, Issue 4, Page(s) e14026

    Abstract: Background: 5-HT: Methods: Non-absorbed 5-HT: Key results: Pharmacological screening demonstrated selectivity and potency of test agonists for 5-HT: Conclusions and inferences: These findings demonstrated that stimulation of epithelial 5- ... ...

    Abstract Background: 5-HT
    Methods: Non-absorbed 5-HT
    Key results: Pharmacological screening demonstrated selectivity and potency of test agonists for 5-HT
    Conclusions and inferences: These findings demonstrated that stimulation of epithelial 5-HT
    MeSH term(s) Animals ; CHO Cells ; Colon/drug effects ; Colon/physiology ; Constipation/drug therapy ; Constipation/physiopathology ; Cricetinae ; Cricetulus ; Gastrointestinal Motility/drug effects ; Gastrointestinal Motility/physiology ; Humans ; Intestinal Mucosa/drug effects ; Intestinal Mucosa/physiology ; Male ; Mice ; Mice, Inbred C57BL ; Mice, Knockout ; Mice, Transgenic ; Receptors, Serotonin, 5-HT4/physiology ; Serotonin 5-HT4 Receptor Agonists/pharmacology ; Serotonin 5-HT4 Receptor Agonists/therapeutic use
    Chemical Substances Serotonin 5-HT4 Receptor Agonists ; Receptors, Serotonin, 5-HT4 (158165-40-3)
    Language English
    Publishing date 2020-11-12
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 1186328-6
    ISSN 1365-2982 ; 1350-1925
    ISSN (online) 1365-2982
    ISSN 1350-1925
    DOI 10.1111/nmo.14026
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 2979: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  2. Article: Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure.

    Lanier, Marion / Pickens, Jason / Bigi, Simone V / Bradshaw-Pierce, Erica L / Chambers, Alison / Cheruvallath, Zacharia S / Cole, Derek / Dougan, Douglas R / Ermolieff, Jacques / Gibson, Tony / Halkowycz, Petro / Hirokawa, Aki / Ivetac, Anthony / Miura, Joanne / Nunez, Evan / Sabat, Mark / Tyhonas, John / Wang, Haixia / Wang, Xiaolun /
    Swann, Steve

    ACS medicinal chemistry letters

    2017  Volume 8, Issue 3, Page(s) 316–320

    Abstract: Apoptosis signal-regulating kinase 1 (ASK1/MAP3K) is a mitogen-activated protein kinase family member shown to contribute to acute ischemia/reperfusion injury. Using structure-based drug design, deconstruction, and reoptimization of a known ASK1 ... ...

    Abstract Apoptosis signal-regulating kinase 1 (ASK1/MAP3K) is a mitogen-activated protein kinase family member shown to contribute to acute ischemia/reperfusion injury. Using structure-based drug design, deconstruction, and reoptimization of a known ASK1 inhibitor, a lead compound was identified. This compound displayed robust MAP3K pathway inhibition and reduction of infarct size in an isolated perfused heart model of cardiac injury.
    Language English
    Publishing date 2017-02-08
    Publishing country United States
    Document type Journal Article
    ISSN 1948-5875
    ISSN 1948-5875
    DOI 10.1021/acsmedchemlett.6b00481
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Correction to "Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure".

    Lanier, Marion / Pickens, Jason / Bigi, Simone V / Bradshaw-Pierce, Erica L / Chambers, Alison / Cheruvallath, Zacharia S / Cole, Derek / Dougan, Douglas R / Ermolieff, Jacques / Gibson, Tony / Halkowycz, Petro / Hirokawa, Aki / Ivetac, Anthony / McBride, Christopher / Miura, Joanne / Nunez, Evan / Sabat, Mark / Tyhonas, John / Wang, Haixia /
    Wang, Xiaolun / Swann, Steve

    ACS medicinal chemistry letters

    2017  Volume 8, Issue 12, Page(s) 1341

    Abstract: This corrects the article DOI: 10.1021/acsmedchemlett.6b00481.]. ...

    Abstract [This corrects the article DOI: 10.1021/acsmedchemlett.6b00481.].
    Language English
    Publishing date 2017-11-08
    Publishing country United States
    Document type Journal Article ; Published Erratum
    ISSN 1948-5875
    ISSN 1948-5875
    DOI 10.1021/acsmedchemlett.7b00457
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article: Rational design of vitamin D3 analogues which selectively restore activity to a vitamin D receptor mutant associated with rickets.

    Swann, Steve L / Bergh, Joel J / Farach-Carson, M Cindy / Koh, John T

    Organic letters

    2003  Volume 4, Issue 22, Page(s) 3863–3866

    Abstract: formula: see text] Vitamin D3-resistant rickets (VDRR) is associated with mutations to the Vitamin D receptor (VDR) which effect ligand-dependent transactivation. Some VDRR associated mutants directly disrupt ligand binding. Using the reported VDR-1,25- ... ...

    Abstract [formula: see text] Vitamin D3-resistant rickets (VDRR) is associated with mutations to the Vitamin D receptor (VDR) which effect ligand-dependent transactivation. Some VDRR associated mutants directly disrupt ligand binding. Using the reported VDR-1,25-dihydroxy vitamin D3 (1,25(OH)2D3) cocrystal structure, three 1,25(OH)2D3 analogues were designed to uniquely complement the rickets associated mutant VDR(Arg274-->Leu). The three analogues were 17 to 286 times more potent than 1,25(OH)2D3 with the mutant in cell-based assays and did not substantially activate cellular calcium influx.
    MeSH term(s) Calcium/metabolism ; Cell Line ; Cholecalciferol/analogs & derivatives ; Drug Design ; Humans ; Ligands ; Models, Molecular ; Mutation ; Receptors, Calcitriol/drug effects ; Receptors, Calcitriol/genetics ; Rickets/drug therapy ; Rickets/genetics ; Structure-Activity Relationship ; Transcriptional Activation/drug effects
    Chemical Substances Ligands ; Receptors, Calcitriol ; Cholecalciferol (1C6V77QF41) ; Calcium (SY7Q814VUP)
    Language English
    Publishing date 2003-02-15
    Publishing country United States
    Document type Journal Article ; Research Support, U.S. Gov't, P.H.S.
    ISSN 1523-7060
    ISSN 1523-7060
    DOI 10.1021/ol0266931
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article: Structure-based design of selective agonists for a rickets-associated mutant of the vitamin d receptor.

    Swann, Steve L / Bergh, Joel / Farach-Carson, Mary C / Ocasio, Cory A / Koh, John T

    Journal of the American Chemical Society

    2002  Volume 124, Issue 46, Page(s) 13795–13805

    Abstract: The nuclear and steroid hormone receptors function as ligand-dependent transcriptional regulators of diverse sets of genes associated with development and homeostasis. Mutations to the vitamin D receptor (VDR), a member of the nuclear and steroid hormone ...

    Abstract The nuclear and steroid hormone receptors function as ligand-dependent transcriptional regulators of diverse sets of genes associated with development and homeostasis. Mutations to the vitamin D receptor (VDR), a member of the nuclear and steroid hormone receptor family, have been linked to human vitamin D-resistant rickets (hVDRR) and result in high serum 1,25(OH)(2)D(3) concentrations and severe bone underdevelopment. Several hVDRR-associated mutants have been localized to the ligand binding domain of VDR and cause a reduction in or loss of ligand binding and ligand-dependent transactivation function. The missense mutation Arg274 --> Leu causes a >1000-fold reduction in 1,25(OH)(2)D(3) responsiveness and is, therefore, no longer regulated by physiological concentrations of the hormone. In this study, computer-aided molecular design was used to generate a focused library of nonsteroidal analogues of the VDR agonist LG190155 that were uniquely designed to complement the Arg274 --> Leu associated with hVDRR. Half of the designed analogues exhibit substantial activity in the hVDRR-associated mutant, whereas none of the structurally similar control compounds exhibited significant activity. The seven most active designed analogues were more than 16 to 526 times more potent than 1,25(OH)(2)D(3) in the mutant receptor (EC(50) = 3.3-121 nM). Significantly, the analogues are selective for the nuclear VDR and did not stimulate cellular calcium influx, which is associated with activation of the membrane-associated vitamin D receptor.
    MeSH term(s) Biphenyl Compounds/chemistry ; Biphenyl Compounds/pharmacology ; Calcitriol/chemistry ; Calcitriol/pharmacology ; Calcium/metabolism ; Cell Membrane/metabolism ; Cells, Cultured ; Drug Design ; Humans ; Ketones/chemistry ; Ketones/pharmacology ; Models, Molecular ; Monte Carlo Method ; Mutation, Missense ; Receptors, Calcitriol/agonists ; Receptors, Calcitriol/chemistry ; Receptors, Calcitriol/genetics ; Rickets/genetics ; Structure-Activity Relationship ; Transcriptional Activation/drug effects
    Chemical Substances Biphenyl Compounds ; Ketones ; LG190155 ; Receptors, Calcitriol ; Calcitriol (FXC9231JVH) ; Calcium (SY7Q814VUP)
    Language English
    Publishing date 2002-11-20
    Publishing country United States
    Document type Journal Article ; Research Support, U.S. Gov't, P.H.S.
    ZDB-ID 3155-0
    ISSN 1520-5126 ; 0002-7863
    ISSN (online) 1520-5126
    ISSN 0002-7863
    DOI 10.1021/ja0268377
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Bonn / Germany

    Z 4' 55/32: Show issues
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