{"id":6186,"date":"2023-02-17T07:11:03","date_gmt":"2023-02-17T07:11:03","guid":{"rendered":"https:\/\/beta.nanion.de\/resource_library\/2017-effect-of-cisplatin-on-the-transport-activity-of-pii-type-atpases\/"},"modified":"2023-02-17T07:11:03","modified_gmt":"2023-02-17T07:11:03","slug":"2017-effect-of-cisplatin-on-the-transport-activity-of-pii-type-atpases","status":"publish","type":"resource_library","link":"https:\/\/nanion.com\/zh-hans\/resource_library\/2017-effect-of-cisplatin-on-the-transport-activity-of-pii-type-atpases\/","title":{"rendered":"2017 &#8211; Effect of cisplatin on the transport activity of PII-type ATPases"},"content":{"rendered":"<p>Cisplatin (cis-diamminedichlorido-Pt(ii)) is extensively used as a chemotherapeutic agent against various types of tumors. However, cisplatin administration causes serious side effects, including nephrotoxicity, ototoxicity and neurotoxicity. It has been shown that cisplatin can interact with P-type ATPases, e.g., Cu+-ATPases (ATP7A and ATP7B) and Na<sup>+<\/sup>\/K<sup>+<\/sup>-ATPase. Cisplatin-induced inhibition of Na<sup>+<\/sup>\/K<sup>+<\/sup>-ATPase has been related to the nephrotoxic effect of the drug. To investigate the inhibitory effects of cisplatin on the pumping activity of PII-type ATPases, electrical measurements were performed on sarcoplasmic reticulum Ca<sup>2+<\/sup>-ATPase (SERCA) and Na<sup>+<\/sup>\/K<sup>+<\/sup>-ATPase embedded in vesicles\/membrane fragments adsorbed on a solid-supported membrane. We found that cisplatin inhibits SERCA and Na<sup>+<\/sup>\/K<sup>+<\/sup>-ATPase only when administered without a physiological reducing agent (GSH); in contrast, inhibition was also observed in the case of Cu+-ATPases in the presence of 1 mM GSH. Our results indicate that cisplatin is a much stronger inhibitor of SERCA (with an IC<sub>50<\/sub>\u00a0value of 1.3 \u03bcM) than of Na<sup>+<\/sup>\/K<sup>+<\/sup>-ATPase (with an IC<sub>50<\/sub>\u00a0value of 11.1 \u03bcM); moreover, cisplatin inhibition of Na<sup>+<\/sup>\/K<sup>+<\/sup>-ATPase is reversible, whereas it is irreversible in the case of SERCA. In the absence of a physiological substrate, while Cu+-ATPases are able to translocate cisplatin, SERCA and Na<sup>+<\/sup>\/K<sup>+<\/sup>-ATPase do not perform ATP-dependent cisplatin displacement.<\/p>\n","protected":false},"featured_media":0,"template":"","products_tags":[36],"resource_type":[75],"application_areas":[108],"therapeutic_areas":[57,290],"target_categories":[60],"target_families":[344],"targets":[207,208],"resource_keyword":[],"class_list":["post-6186","resource_library","type-resource_library","status-publish","hentry","products_tags-surfe2r-n1","resource_type-publication","application_areas-transporters","therapeutic_areas-cancer","therapeutic_areas-toxicology","target_categories-transporters","target_families-p-type-atpases","targets-serca","targets-na-k-atpase"],"acf":[],"_links":{"self":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_library\/6186","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=6186"}],"wp:term":[{"taxonomy":"products_tags","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/products_tags?post=6186"},{"taxonomy":"resource_type","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_type?post=6186"},{"taxonomy":"application_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/application_areas?post=6186"},{"taxonomy":"therapeutic_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/therapeutic_areas?post=6186"},{"taxonomy":"target_categories","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_categories?post=6186"},{"taxonomy":"target_families","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_families?post=6186"},{"taxonomy":"targets","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/targets?post=6186"},{"taxonomy":"resource_keyword","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_keyword?post=6186"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}