{"id":6131,"date":"2023-02-17T07:02:39","date_gmt":"2023-02-17T07:02:39","guid":{"rendered":"https:\/\/beta.nanion.de\/resource_library\/2015-the-functional-property-changes-of-muscular-nav1-4-and-cardiac-nav1-5-induced-by-scorpion-toxin-bmk-agp-sypu1-mutants-y42f-and-y5f\/"},"modified":"2023-02-17T07:02:39","modified_gmt":"2023-02-17T07:02:39","slug":"2015-the-functional-property-changes-of-muscular-nav1-4-and-cardiac-nav1-5-induced-by-scorpion-toxin-bmk-agp-sypu1-mutants-y42f-and-y5f","status":"publish","type":"resource_library","link":"https:\/\/nanion.com\/zh-hans\/resource_library\/2015-the-functional-property-changes-of-muscular-nav1-4-and-cardiac-nav1-5-induced-by-scorpion-toxin-bmk-agp-sypu1-mutants-y42f-and-y5f\/","title":{"rendered":"2015 &#8211; The Functional Property Changes of Muscular NaV1.4 and Cardiac NaV1.5 Induced by Scorpion Toxin BmK AGP-SYPU1 Mutants Y42F and Y5F"},"content":{"rendered":"<p>Scorpion toxins are invaluable therapeutic leads and pharmacological tools which influence the voltage-gated sodium channels. However, the details were still unclear about the structure\u2013function relationship of scorpion toxins on VGSC subtypes. In the previous study, we reported one \u03b1-type scorpion toxin Bmk AGP-SYPU1 and its two mutants (Y5F and Y42F) which had been demonstrated to ease pain in mice acetic acid writhing test. However, the function of Bmk AGP-SYPU1 on VGSCs is still unknown. In this study, we examined the effects of BmK AGP-SYPU1 and its two mutants (Y5F and Y42F) on hNaV1.4 and hNaV1.5 heterologously expressed CHO cell lines by using Na<sup>+<\/sup>-specialized fluorescent dye and whole-cell patch clamp. The data showed that BmK AGP-SYPU1 displayed as an activator of hNaV1.4 and hNaV1.5, which might indeed contribute to its biotoxicity to muscular and cardiac system and exhibited the functional properties of both the \u03b1-type and \u03b2-type scorpion toxin. Notably, Y5F mutant exhibited lower activatory effects on hNaV1.4 and hNaV1.5 compared with BmK AGP-SYPU1. Y42F was an enhanced activator and confirmed that the conserved Tyr42 was the key amino acid involved in bioactivity or biotoxicity. These data provided a deep insight into the structure\u2013function relationship of BmK AGP-SYPU1, which may be the guidance for engineering \u03b1-toxin with high selectivity on VGSC subtypes.<\/p>\n","protected":false},"featured_media":0,"template":"","products_tags":[45],"resource_type":[75],"application_areas":[50,76],"therapeutic_areas":[56],"target_categories":[61],"target_families":[332],"targets":[93,263],"resource_keyword":[],"class_list":["post-6131","resource_library","type-resource_library","status-publish","hentry","products_tags-port-a-patch","resource_type-publication","application_areas-ion-channels","application_areas-drug-discovery","therapeutic_areas-pain","target_categories-voltage-gated-ion-channels","target_families-nav-channels","targets-nav1-5","targets-nav1-4"],"acf":[],"_links":{"self":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_library\/6131","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_library"}],"about":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/types\/resource_library"}],"wp:attachment":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/media?parent=6131"}],"wp:term":[{"taxonomy":"products_tags","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/products_tags?post=6131"},{"taxonomy":"resource_type","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_type?post=6131"},{"taxonomy":"application_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/application_areas?post=6131"},{"taxonomy":"therapeutic_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/therapeutic_areas?post=6131"},{"taxonomy":"target_categories","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_categories?post=6131"},{"taxonomy":"target_families","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_families?post=6131"},{"taxonomy":"targets","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/targets?post=6131"},{"taxonomy":"resource_keyword","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_keyword?post=6131"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}