VSE knjižnice (vzajemna bibliografsko-kataložna baza podatkov COBIB.SI)
  • Design and characterization of a novel structural class of Kv1.3 inhibitors
    Hendrickx, Louise Antonia ...
    The voltage-gated potassium channel Kv1.3 is involved in multiple autoimmune diseases, such as multiple sclerosis, rheumatoid arthritis, diabetes mellitus type 1 and psoriasis. In many auto-immune ... diseases better treatment options are desired as existing therapies are often ineffective or become less effective over time, for which Kv1.3 inhibitors arise as promising candidates. In this study, five compounds were selected based on a 3D similarity searching methodology and subsequently screened ex vivo on the Kv1.3 channel. The screening resulted in two compounds inhibiting the Kv1.3 channel, of which TVS-12 was the most potent compound, while TVS-06 -although less potent- showed an excellent selectivity for Kv1.3. For both compounds the mechanism of action was investigated by an electrophysiological characterization on the Kv1.3 channel and three Kv1.3 mutants, designed to resemble the pore region of Kv1.2 channels. Structurally, the presence of a benzene ring and/or an oxane ring seems to cause a better interaction with the Kv1.3 channel, resulting in a 20-fold higher potency for TVS-12.
    Vir: Bioorganic chemistry. - ISSN 0045-2068 (Vol. 98, 2020, str. 1-9)
    Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasle
    Leto - 2020
    Jezik - angleški
    COBISS.SI-ID - 4895857

    Povezava(-e):

    https://www.sciencedirect.com/science/article/pii/S0045206819321418
    DOI

Vnos na polico