{"id":13421,"date":"2024-01-17T11:05:20","date_gmt":"2024-01-17T11:05:20","guid":{"rendered":"https:\/\/www.nanion.de\/?post_type=resource_library&#038;p=13421"},"modified":"2024-01-17T11:41:10","modified_gmt":"2024-01-17T11:41:10","slug":"2024-unraveling-the-kinetics-and-pharmacology-of-human-pept1-using-solid-supported-membrane-based-electrophysiology","status":"publish","type":"resource_library","link":"https:\/\/nanion.com\/ja\/resource_library\/2024-unraveling-the-kinetics-and-pharmacology-of-human-pept1-using-solid-supported-membrane-based-electrophysiology\/","title":{"rendered":"2024 &#8211; Unraveling the kinetics and pharmacology of human PepT1 using solid supported membrane-based electrophysiology"},"content":{"rendered":"<p>The human Peptide Transporter 1 (hPepT1) is known for its broad substrate specificity and its ability to transport (pro-)drugs. Here, we present an in-depth comprehensive study of hPepT1 and its interactions with various substrates via solid supported membrane-based electrophysiology (SSME). Using hPepT1-containing vesicles, we could not identify any peptide induced pre-steady-state currents, indicating that the recorded peak currents reflect steady-state transport. Electrogenic co-transport of H<sup>+<\/sup>\/glycylglycine (GlyGly) was observed across a pH range of 5.0 to 9.0. The pH dependence is described by a bell-shaped activity curve and two pK values. K<sub>M<\/sub>\u00a0and relative V<sub>max<\/sub>\u00a0values of various canonical and non-canonical peptide substrates were contextualized with current mechanistic understandings of hPepT1. Finally, specific inhibition was observed for various inhibitors in a high throughput format, and IC50 values are reported. Taken together, these findings contribute to promoting the design and analysis of pharmacologically relevant substances.<\/p>\n","protected":false},"featured_media":0,"template":"","products_tags":[36,132],"resource_type":[75],"application_areas":[53,108],"therapeutic_areas":[143],"target_categories":[60],"target_families":[375],"targets":[136],"resource_keyword":[],"class_list":["post-13421","resource_library","type-resource_library","status-publish","hentry","products_tags-surfe2r-n1","products_tags-surfe2r-96se","resource_type-publication","application_areas-assay-development-and-validation","application_areas-transporters","therapeutic_areas-assay-development-and-validation","target_categories-transporters","target_families-symporter","targets-pept1-slc15a1"],"acf":[],"_links":{"self":[{"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/resource_library\/13421","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/resource_library"}],"about":[{"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/types\/resource_library"}],"wp:attachment":[{"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/media?parent=13421"}],"wp:term":[{"taxonomy":"products_tags","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/products_tags?post=13421"},{"taxonomy":"resource_type","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/resource_type?post=13421"},{"taxonomy":"application_areas","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/application_areas?post=13421"},{"taxonomy":"therapeutic_areas","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/therapeutic_areas?post=13421"},{"taxonomy":"target_categories","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/target_categories?post=13421"},{"taxonomy":"target_families","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/target_families?post=13421"},{"taxonomy":"targets","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/targets?post=13421"},{"taxonomy":"resource_keyword","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/resource_keyword?post=13421"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}