LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 4 of total 4

Search options

  1. Article ; Online: DNA-Compatible Conditions for the Formation of

    Zhang, Panpan / Koch, Grant / Zhang, Yankun / Yang, Kevin / Lokey, R Scott

    ACS omega

    2023  Volume 8, Issue 26, Page(s) 23477–23483

    Abstract: DNA-encoded libraries (DELs) are a powerful platform in drug discovery. Peptides have unique properties that make them attractive pharmaceutical candidates. N-methylation of the peptide backbone can confer beneficial properties such as increased ... ...

    Abstract DNA-encoded libraries (DELs) are a powerful platform in drug discovery. Peptides have unique properties that make them attractive pharmaceutical candidates. N-methylation of the peptide backbone can confer beneficial properties such as increased proteolytic stability and membrane permeability. Herein, we evaluate different DEL reaction systems and report a DNA-compatible protocol for forming N-methylated amide bonds. The DNA-compatible, bis(trichloromethyl)carbonate-mediated amide coupling is efficient for the formation of N-methyl peptide bonds, which promises to increase the opportunity to identify passively cell-permeable macrocyclic peptide hits by DNA-encoded technology.
    Language English
    Publishing date 2023-06-20
    Publishing country United States
    Document type Journal Article
    ISSN 2470-1343
    ISSN (online) 2470-1343
    DOI 10.1021/acsomega.3c00576
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

  2. Article ; Online: Reevaluation of a Bicyclic Pyrazoline as a Selective 15-Lipoxygenase V-Type Activator Possessing Fatty Acid Specificity.

    van Hoorebeke, Christopher / Yang, Kevin / Mussetter, Samuel J / Koch, Grant / Rutz, Natalie / Lokey, R Scott / Crews, Phillip / Holman, Theodore R

    ACS omega

    2022  Volume 7, Issue 47, Page(s) 43169–43179

    Abstract: Regulation of lipoxygenase (LOX) activity is of great interest due to the involvement of the various LOX isoforms in the inflammatory process and hence many diseases. The bulk of investigations have centered around the discovery and design of inhibitors. ...

    Abstract Regulation of lipoxygenase (LOX) activity is of great interest due to the involvement of the various LOX isoforms in the inflammatory process and hence many diseases. The bulk of investigations have centered around the discovery and design of inhibitors. However, the emerging understanding of the role of h15-LOX-1 in the resolution of inflammation provides a rationale for the development of activators as well. Bicyclic pyrazolines are known bioactive molecules that have been shown to display antibiotic and anti-inflammatory activities. In the current work, we reevaluated a previously discovered bicyclic pyrazoline h15-LOX-1 activator, PKUMDL_MH_1001 (written as
    Language English
    Publishing date 2022-11-17
    Publishing country United States
    Document type Journal Article
    ISSN 2470-1343
    ISSN (online) 2470-1343
    DOI 10.1021/acsomega.2c05877
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

  3. Article ; Online: StARD9 is a novel lysosomal kinesin required for membrane tubulation, cholesterol transport and Purkinje cell survival.

    Sterling, Felicity R / D'Amico, Jon / Brumfield, Alexandria M / Huegel, Kara L / Vaughan, Patricia S / Morris, Kathryn / Schwarz, Shelby / Joyce, Michelle V / Boggess, Bill / Champion, Matthew M / Maciuba, Kevin / Allen, Philip / Marasco, Eric / Koch, Grant / Gonzalez, Peter / Hodges, Shannon / Leahy, Shannon / Gerstbauer, Erica / Hinchcliffe, Edward H /
    Vaughan, Kevin T

    Journal of cell science

    2023  Volume 136, Issue 5

    Abstract: The pathological accumulation of cholesterol is a signature feature of Niemann-Pick type C (NPC) disease, in which excessive lipid levels induce Purkinje cell death in the cerebellum. NPC1 encodes a lysosomal cholesterol-binding protein, and mutations in ...

    Abstract The pathological accumulation of cholesterol is a signature feature of Niemann-Pick type C (NPC) disease, in which excessive lipid levels induce Purkinje cell death in the cerebellum. NPC1 encodes a lysosomal cholesterol-binding protein, and mutations in NPC1 drive cholesterol accumulation in late endosomes and lysosomes (LE/Ls). However, the fundamental role of NPC proteins in LE/L cholesterol transport remains unclear. Here, we demonstrate that NPC1 mutations impair the projection of cholesterol-containing membrane tubules from the surface of LE/Ls. A proteomic survey of purified LE/Ls identified StARD9 as a novel lysosomal kinesin responsible for LE/L tubulation. StARD9 contains an N-terminal kinesin domain, a C-terminal StART domain, and a dileucine signal shared with other lysosome-associated membrane proteins. Depletion of StARD9 disrupts LE/L tubulation, paralyzes bidirectional LE/L motility and induces accumulation of cholesterol in LE/Ls. Finally, a novel StARD9 knock-out mouse recapitulates the progressive loss of Purkinje cells in the cerebellum. Together, these studies identify StARD9 as a microtubule motor protein responsible for LE/L tubulation and provide support for a novel model of LE/L cholesterol transport that becomes impaired in NPC disease.
    MeSH term(s) Animals ; Mice ; Purkinje Cells ; Kinesins/genetics ; Proteomics ; Biological Transport ; Lysosomes ; Mice, Knockout
    Chemical Substances Kinesins (EC 3.6.4.4)
    Language English
    Publishing date 2023-03-02
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S.
    ZDB-ID 2993-2
    ISSN 1477-9137 ; 0021-9533
    ISSN (online) 1477-9137
    ISSN 0021-9533
    DOI 10.1242/jcs.260662
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 1200: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)
    Zs.MG 14: Show issues

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  4. Article ; Online: Synthesis and Structure-Activity Relationship of Dual-Stage Antimalarial Pyrazolo[3,4-

    Eagon, Scott / Hammill, Jared T / Sigal, Martina / Ahn, Kevin J / Tryhorn, Julia E / Koch, Grant / Belanger, Briana / Chaplan, Cory A / Loop, Lauren / Kashtanova, Anna S / Yniguez, Kenya / Lazaro, Horacio / Wilkinson, Steven P / Rice, Amy L / Falade, Mofolusho O / Takahashi, Rei / Kim, Katie / Cheung, Ashley / DiBernardo, Celine /
    Kimball, Joshua J / Winzeler, Elizabeth A / Eribez, Korina / Mittal, Nimisha / Gamo, Francisco-Javier / Crespo, Benigno / Churchyard, Alisje / García-Barbazán, Irene / Baum, Jake / Anderson, Marc O / Laleu, Benoît / Guy, R Kiplin

    Journal of medicinal chemistry

    2020  Volume 63, Issue 20, Page(s) 11902–11919

    Abstract: Malaria remains one of the most deadly infectious diseases, causing hundreds of thousands of deaths each year, primarily in young children and pregnant mothers. Here, we report the discovery and derivatization of a series of pyrazolo[3,4- ...

    Abstract Malaria remains one of the most deadly infectious diseases, causing hundreds of thousands of deaths each year, primarily in young children and pregnant mothers. Here, we report the discovery and derivatization of a series of pyrazolo[3,4-
    MeSH term(s) Antimalarials/chemical synthesis ; Antimalarials/chemistry ; Antimalarials/pharmacology ; Cell Line ; Dose-Response Relationship, Drug ; Hep G2 Cells ; Humans ; Models, Molecular ; Molecular Structure ; Parasitic Sensitivity Tests ; Plasmodium falciparum/drug effects ; Pyrazoles/chemical synthesis ; Pyrazoles/chemistry ; Pyrazoles/pharmacology ; Pyridines/chemical synthesis ; Pyridines/chemistry ; Pyridines/pharmacology ; Structure-Activity Relationship
    Chemical Substances Antimalarials ; Pyrazoles ; Pyridines ; pyrazolo(3,4-b)pyridine
    Language English
    Publishing date 2020-10-01
    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.0c01152
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    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)
    Zs.MB 1: Show issues

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

To top