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  1. Article ; Online: Optimization of Orally Bioavailable Antileishmanial 2,4,5-Trisubstituted Benzamides.

    Kim, Ho Shin / Ortiz, Diana / Kadayat, Tara Man / Fargo, Corinne M / Hammill, Jared T / Chen, Yizhe / Rice, Amy L / Begley, Kristin L / Shoeran, Gaurav / Pistel, William / Yates, Phillip A / Sanchez, Marco A / Landfear, Scott M / Guy, R Kiplin

    Journal of medicinal chemistry

    2023  Volume 66, Issue 11, Page(s) 7374–7386

    Abstract: Leishmaniasis, a neglected tropical disease caused ... ...

    Abstract Leishmaniasis, a neglected tropical disease caused by
    MeSH term(s) Humans ; Animals ; Mice ; Leishmania ; Leishmaniasis/drug therapy ; Leishmaniasis/chemically induced ; Leishmaniasis/parasitology ; Antiprotozoal Agents/chemistry ; Benzamides/pharmacology ; Benzamides/therapeutic use
    Chemical Substances benzamide (6X80438640) ; Antiprotozoal Agents ; Benzamides
    Language English
    Publishing date 2023-05-22
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.3c00056
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

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  2. Article ; Online: Improvement of Oral Bioavailability of Pyrazolo-Pyridone Inhibitors of the Interaction of DCN1/2 and UBE2M.

    Kim, Ho Shin / Hammill, Jared T / Scott, Daniel C / Chen, Yizhe / Rice, Amy L / Pistel, William / Singh, Bhuvanesh / Schulman, Brenda A / Guy, R Kiplin

    Journal of medicinal chemistry

    2021  Volume 64, Issue 9, Page(s) 5850–5862

    Abstract: The cullin-RING ubiquitin ligases (CRLs) are ubiquitin E3 enzymes that play a key role in controlling proteasomal degradation and are activated by neddylation. We previously reported inhibitors that target CRL activation by disrupting the interaction of ... ...

    Abstract The cullin-RING ubiquitin ligases (CRLs) are ubiquitin E3 enzymes that play a key role in controlling proteasomal degradation and are activated by neddylation. We previously reported inhibitors that target CRL activation by disrupting the interaction of defective in cullin neddylation 1 (DCN1), a CRL neddylation co-E3, and UBE2M, a neddylation E2. Our first-generation inhibitors possessed poor oral bioavailability and fairly rapid clearance that hindered the study of acute inhibition of DCN-controlled CRL activity in vivo. Herein, we report studies to improve the pharmacokinetic performance of the pyrazolo-pyridone inhibitors. The current best inhibitor,
    MeSH term(s) Administration, Oral ; Animals ; Binding Sites ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Crystallography, X-Ray ; Drug Design ; Drug Stability ; Half-Life ; Humans ; Intracellular Signaling Peptides and Proteins/antagonists & inhibitors ; Intracellular Signaling Peptides and Proteins/metabolism ; Mice ; Molecular Dynamics Simulation ; Pyrazoles/chemistry ; Pyrazoles/metabolism ; Pyrazoles/pharmacology ; Pyridines/chemistry ; Pyridines/metabolism ; Pyridines/pharmacology ; Structure-Activity Relationship ; Ubiquitin-Conjugating Enzymes/antagonists & inhibitors ; Ubiquitin-Conjugating Enzymes/metabolism
    Chemical Substances DCUN1D1 protein, human ; Intracellular Signaling Peptides and Proteins ; Pyrazoles ; Pyridines ; pyrazolopyridine ; Ubiquitin-Conjugating Enzymes (EC 2.3.2.23) ; UBE2M protein, human (EC 6.3.2.-)
    Language English
    Publishing date 2021-05-04
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.1c00035
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
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    Order via subito

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