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  • Immunosuppressive effects of new thiophene-based K▫$_V$▫1.3 inhibitors
    Gubič, Špela ...
    Voltage-gated potassium channel KV1.3 inhibitors have been shown to be effective in preventing T-cell proliferation and activation by affecting intracellular Ca2+ homeostasis. Here, we present the ... structure-activity relationship, KV1.3 inhibition, and immunosuppressive effects of new thiophene-based KV1.3 inhibitors with nanomolar potency on K+ current in T-lymphocytes and KV1.3 inhibition on Ltk− cells. The new KV1.3 inhibitor trans-18 inhibited KV1.3 -mediated current in phytohemagglutinin (PHA)-activated T-lymphocytes with an IC50 value of 26.1 nM and in mammalian Ltk− cells with an IC50 value of 230 nM. The KV1.3 inhibitor trans-18 also had nanomolar potency against KV1.3 in Xenopus laevis oocytes (IC50 = 136 nM). The novel thiophene-based KV1.3 inhibitors impaired intracellular Ca2+ signaling as well as T-cell activation, proliferation, and colony formation.
    Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 259, art. 115561, 2023, 17 str.)
    Type of material - article, component part ; adult, serious
    Publish date - 2023
    Language - english
    COBISS.SI-ID - 156924419

    Link(s):

    https://www.sciencedirect.com/science/article/pii/S0223523423005275
    Repository of the University of Ljubljana – RUL
    DOI

source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 259, art. 115561, 2023, 17 str.)

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