{"id":6086,"date":"2023-02-17T07:10:36","date_gmt":"2023-02-17T07:10:36","guid":{"rendered":"https:\/\/beta.nanion.de\/resource_library\/2014-anticancer-rutheniumiii-complex-kp1019-interferes-with-atp-dependent-ca2-translocation-by-sarco-endoplasmic-reticulum-ca2-atpase-serca\/"},"modified":"2023-02-17T07:10:36","modified_gmt":"2023-02-17T07:10:36","slug":"2014-anticancer-rutheniumiii-complex-kp1019-interferes-with-atp-dependent-ca2-translocation-by-sarco-endoplasmic-reticulum-ca2-atpase-serca","status":"publish","type":"resource_library","link":"https:\/\/nanion.com\/zh-hans\/resource_library\/2014-anticancer-rutheniumiii-complex-kp1019-interferes-with-atp-dependent-ca2-translocation-by-sarco-endoplasmic-reticulum-ca2-atpase-serca\/","title":{"rendered":"2014 &#8211; Anticancer Ruthenium(III) Complex KP1019 Interferes with ATP-Dependent Ca<sup>2+<\/sup> Translocation by Sarco-Endoplasmic Reticulum Ca<sup>2+<\/sup>-ATPase (SERCA)"},"content":{"rendered":"<p>Sarco-endoplasmic reticulum Ca<sup>2+<\/sup>-ATPase (SERCA), a P-type ATPase that sustains Ca<sup>2+<\/sup>\u00a0transport and plays a major role in intracellular Ca<sup>2+<\/sup>\u00a0homeostasis, represents a therapeutic target for cancer therapy. Here, we investigated whether ruthenium-based anticancer drugs, namely KP1019 (indazolium [trans-tetrachlorobis(1H-indazole)ruthenate(III)]), NAMI-A (imidazolium [trans-tetrachloro(1H-imidazole)(S-dimethylsulfoxide)ruthenate(III)]) and RAPTA-C ([Ru(\u03b76-p-cymene)dichloro(1,3,5-triaza-7-phosphaadamantane)]), and cisplatin (cis-diammineplatinum(II) dichloride) might act as inhibitors of SERCA. Charge displacement by SERCA adsorbed on a solid-supported membrane was measured after ATP or Ca<sup>2+<\/sup>\u00a0concentration jumps. Our results show that KP1019, in contrast tocancer the other metal compounds, is able to interfere with ATP-dependent translocation of Ca<sup>2+<\/sup>\u00a0ions. An IC<sub>50<\/sub>\u00a0value of 1\u2005\u03bcM\u00a0was determined for inhibition of calcium translocation by KP1019. Conversely, it appears that KP1019 does not significantly affect Ca<sup>2+<\/sup>\u00a0binding to the ATPase from the cytoplasmic side. Inhibition of SERCA at pharmacologically relevant concentrations may represent a crucial aspect in the overall pharmacological and toxicological profile of KP1019.<\/p>\n","protected":false},"featured_media":0,"template":"","products_tags":[36],"resource_type":[75],"application_areas":[108],"therapeutic_areas":[],"target_categories":[60],"target_families":[344],"targets":[207],"resource_keyword":[],"class_list":["post-6086","resource_library","type-resource_library","status-publish","hentry","products_tags-surfe2r-n1","resource_type-publication","application_areas-transporters","target_categories-transporters","target_families-p-type-atpases","targets-serca"],"acf":[],"_links":{"self":[{"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_library\/6086","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=6086"}],"wp:term":[{"taxonomy":"products_tags","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/products_tags?post=6086"},{"taxonomy":"resource_type","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_type?post=6086"},{"taxonomy":"application_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/application_areas?post=6086"},{"taxonomy":"therapeutic_areas","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/therapeutic_areas?post=6086"},{"taxonomy":"target_categories","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_categories?post=6086"},{"taxonomy":"target_families","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/target_families?post=6086"},{"taxonomy":"targets","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/targets?post=6086"},{"taxonomy":"resource_keyword","embeddable":true,"href":"https:\/\/nanion.com\/zh-hans\/wp-json\/wp\/v2\/resource_keyword?post=6086"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}