{"id":12170,"date":"2023-07-28T14:38:55","date_gmt":"2023-07-28T14:38:55","guid":{"rendered":"https:\/\/www.nanion.de\/?post_type=resource_library&#038;p=12170"},"modified":"2023-07-28T14:38:55","modified_gmt":"2023-07-28T14:38:55","slug":"2023-structure-function-relationship-of-new-peptides-activating-human-nav1-1","status":"publish","type":"resource_library","link":"https:\/\/nanion.com\/zh-hans\/resource_library\/2023-structure-function-relationship-of-new-peptides-activating-human-nav1-1\/","title":{"rendered":"2023 &#8211; Structure-function relationship of new peptides activating human Nav1.1"},"content":{"rendered":"<p>Na<sub>v<\/sub>1.1 is an important\u00a0pharmacological target\u00a0as this voltage-gated sodium channel is involved in neurological and cardiac syndromes. Channel activators are actively sought to try to compensate for\u00a0haploinsufficiency\u00a0in several of these pathologies. Herein we used a natural source of new peptide compounds active on ion channels and screened for\u00a0drugs\u00a0capable to inhibit channel inactivation as a way to compensate for decreased channel function. We discovered that JzTx-34 is highly active on Na<sub>v<\/sub>1.1 and subsequently performed a full structure-activity relationship investigation to identify its\u00a0pharmacophore. These experiments will help interpret the mechanism of action of this and formerly identified peptides as well as the future identification of new peptides. We also reveal structural determinants that make natural\u00a0ICK\u00a0peptides active against Na<sub>v<\/sub>1.1 challenging to synthesize. Altogether, the knowledge gained by this study will help facilitate the discovery and development of new compounds active on this critical ion channel target.<\/p>\n<p>&nbsp;<\/p>\n<p>Read more in the publication <a href=\"https:\/\/www.sciencedirect.com\/science\/article\/pii\/S0753332223009642\">here<\/a>.<\/p>\n","protected":false},"featured_media":0,"template":"","products_tags":[42],"resource_type":[75],"application_areas":[50,53,76],"therapeutic_areas":[54,55,143],"target_categories":[61],"target_families":[332],"targets":[234],"resource_keyword":[],"class_list":["post-12170","resource_library","type-resource_library","status-publish","hentry","products_tags-syncropatch-384","resource_type-publication","application_areas-ion-channels","application_areas-assay-development-and-validation","application_areas-drug-discovery","therapeutic_areas-cardiac-safety-cipa","therapeutic_areas-cns","therapeutic_areas-assay-development-and-validation","target_categories-voltage-gated-ion-channels","target_families-nav-channels","targets-nav1-1"],"acf":[],"_links":{"self":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_library\/12170","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=12170"}],"wp:term":[{"taxonomy":"products_tags","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/products_tags?post=12170"},{"taxonomy":"resource_type","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_type?post=12170"},{"taxonomy":"application_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/application_areas?post=12170"},{"taxonomy":"therapeutic_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/therapeutic_areas?post=12170"},{"taxonomy":"target_categories","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_categories?post=12170"},{"taxonomy":"target_families","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_families?post=12170"},{"taxonomy":"targets","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/targets?post=12170"},{"taxonomy":"resource_keyword","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_keyword?post=12170"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}