{"id":16980,"date":"2025-03-07T07:16:59","date_gmt":"2025-03-07T07:16:59","guid":{"rendered":"https:\/\/www.nanion.de\/?post_type=resource_library&#038;p=16980"},"modified":"2025-03-07T07:16:59","modified_gmt":"2025-03-07T07:16:59","slug":"2025-photo-isomerization-of-azobenzene-extended-charybdotoxin-for-the-optical-control-of-kv1-2-potassium-channel-activity","status":"publish","type":"resource_library","link":"https:\/\/nanion.com\/zh-hans\/resource_library\/2025-photo-isomerization-of-azobenzene-extended-charybdotoxin-for-the-optical-control-of-kv1-2-potassium-channel-activity\/","title":{"rendered":"2025 &#8211; Photo-isomerization of azobenzene-extended charybdotoxin for the optical control of Kv1.2 potassium channel activity"},"content":{"rendered":"<p>Natural peptides from animal venoms effectively modulate ion channel activity. While photoswitches regulate small compound pharmacology, their application to\u00a0natural\u00a0peptides\u00a0rich in disulfide bridges and active on ion channels\u00a0is novel due to larger pharmacophores. We initiated a pilot study integrating azobenzene photoswitches into charybdotoxin (ChTx), known for blocking potassium channels.\u00a0Two click-chemistry-compatible azobenzene were synthesized differing in length and amide orientation (Az1\u00a0&amp; Az2).\u00a0Az1\u00a0was\u00a0grafted onto ChTx at various amino acid positions using L-azidohomoalanine mutation. ChTx monomers outperformed dimers, particularly with azobenzene at position 14, by exhibiting optimal photoswitching activity. In the\u00a0cis\u00a0configuration,\u00a0Az1\u00a0altered ChTx&#8217;s pharmacophore, reducing potassium channel blockage,\u00a0while conversely Az2\u00a0increased ChTx potency. This study pioneers photoswitch application to complex peptides, leveraging structure-activity relationships. Successful integration depends on precise azobenzene positioning and chemical grafting guided by SAR insights. This advancement underscores the adaptability of photoswitch technology to intricate peptide structures, offering new avenues for pharmacological modulation.<\/p>\n","protected":false},"featured_media":0,"template":"","products_tags":[42],"resource_type":[75],"application_areas":[50,53],"therapeutic_areas":[143],"target_categories":[61],"target_families":[333],"targets":[284],"resource_keyword":[],"class_list":["post-16980","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","therapeutic_areas-assay-development-and-validation","target_categories-voltage-gated-ion-channels","target_families-kv-channels","targets-kv1-2"],"acf":[],"_links":{"self":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_library\/16980","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=16980"}],"wp:term":[{"taxonomy":"products_tags","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/products_tags?post=16980"},{"taxonomy":"resource_type","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_type?post=16980"},{"taxonomy":"application_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/application_areas?post=16980"},{"taxonomy":"therapeutic_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/therapeutic_areas?post=16980"},{"taxonomy":"target_categories","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_categories?post=16980"},{"taxonomy":"target_families","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_families?post=16980"},{"taxonomy":"targets","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/targets?post=16980"},{"taxonomy":"resource_keyword","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_keyword?post=16980"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}