IndraLab

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SHPK inhibits KCNA3. 21 / 21
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"Stichodactyla toxin (ShK), isolated from the sea anemone Stichodactyla helianthus, is a potent blocker of Kv1.3."
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"ShK is able to block Kv1.3 at low picomolar concentrations."
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"Therefore, we also tested ShK toxin which is described to be highly specific for the block of Kv1.3 channels."
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"The sea anemone venom protein ShK of Stichodactyla helianthus inhibited Kv1.3 with an IC50 in the low picomolar range ."
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"Dalazatide (ShK-186), an analog of the sea anemone toxin ShK, blocks Kv1.3 with picomolar affinity and specificity."
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"ShK was used as a control and found to inhibit Kv1.3 with an IC of 57 pM (data not shown), replicating the low picomolar values described in the previous literature (19)."
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"ShK or its derivatives block Kv1.3 with high selectivity over other Kv channels , and show efficacy in rat models of autoimmune conditions including arthritis , diabetes , dermatitis , and asthma ."
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"Electrophysiological studies on ShK and the closely-related peptide HmK show that ShK blocks K V 1.3 with significantly higher potency, even though molecular dynamics simulations show that ShK is more flexible than HmK."
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"Lymphocytes have voltage-gated potassium channel Kv1.3 that can be inhibited by polypeptide toxin homolog (ShK) found among the helminths like AcK1 in Ancylostoma caninum and A. ceylanicum, BmK1 in B.[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"ShK blocks the Kv1.3 channel at picomolar concentrations (Beeton et al., 2006; 2011)."
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"Although it inhibits several KV subtypes , ShK most potently blocks KV1.3 with an IC50 of ~ 10 pM ."
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"Kv1.3 channels can be selectively inhibited by synthetic analogues of a native ShK toxin isolated from the sea anemone Stichodactyla helianthus."
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"Engineered variants of ShK, OsK1 and OdK2 that potently and selectively inhibit Kv1.3 have also been identified [ xref , xref ]."
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"The ShK peptide derived from Stichodactyla toxin has been known to block the pore region of eukaryotic Kv1.3 by interacting with all the four subunits of tetrameric Kv1.3 [ 23 ], and it can suppress t[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"These results suggest that the Kv1.3 suppressor ShK alleviates DMM‐induced cartilage erosion by inhibiting M1 polarization macrophage‐mediated activation in vitro.2.3 Inhibition of Kv1.3 Effectively Inhibits OA Progression In Vitro and In Vivo."
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"For instance, ShK-related peptides derived from parasitic worms, such as AcK1 and BmK1, have been shown to block Kv1.3 channels and suppress T cell responses in vitro and in vivo [37]."
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"To further investigate whether the secreted ShK from ShK‐UCMSCs can inhibit Kv1.3 channels on RAW264.7cells, we cocultured LPS pretreated RAW264.7 macrophages with vehicle control vel‐UCMSCs or ShK‐UCMSCs."
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"As described previously [ xref , xref ], ShK inhibited Kv1.3 and Kv1.1 channels with similar potencies (IC 50 of 9 ± 2 pM for Kv1.3 and 23 ± 3 pM for Kv1.1)."
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"In contrast, we have also found that the chimeric SAK1 toxin Hui1 and the natural toxin ShK blocked KcsA and Kv1.3 using an arginine residue, Hui1-Arg and ShK-Arg , respectively, two positions past the canonical blocking lysine, indicative of an alternative binding orientation (10)."
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"100 nm ShK (QYAOBIO, Shanghai, China) was added to inhibit Kv1.3 to assess the role of Kv1.3 channels in M1 macrophage polarization."
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"STH secrete immunoregulatory molecules that act directly on T cells, typified by the hookworm homologues of sea anemone ShK toxins that block Kv1.3 voltage-gated potassium channels and are crucial for the activation of effector memory T cells (Smallwood et al., 2021)."
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