{"id":11391,"date":"2023-06-09T07:20:24","date_gmt":"2023-06-09T07:20:24","guid":{"rendered":"https:\/\/www.nanion.de\/?post_type=resource_library&#038;p=11391"},"modified":"2024-01-17T08:52:03","modified_gmt":"2024-01-17T08:52:03","slug":"2023-modulators-of-cellular-cholesterol-homeostasis-as-antiproliferative-and-model-membranes-perturbing-agents","status":"publish","type":"resource_library","link":"https:\/\/nanion.com\/ja\/resource_library\/2023-modulators-of-cellular-cholesterol-homeostasis-as-antiproliferative-and-model-membranes-perturbing-agents\/","title":{"rendered":"2023 &#8211; Modulators of cellular cholesterol homeostasis as antiproliferative and model membranes perturbing agents"},"content":{"rendered":"<p>Cholesterol is an important component of\u00a0mammalian cell\u00a0membranes affecting their fluidity and permeability. Together with\u00a0sphingomyelin, cholesterol forms microdomains, called\u00a0lipid rafts. They play important role in\u00a0signal transduction\u00a0forming platforms for interaction of signal proteins. Altered levels of cholesterol are known to be strongly associated with the development of various pathologies (e.g., cancer, atherosclerosis and cardiovascular diseases). In the present work, the group of compounds that share the property of affecting cellular\u00a0homeostasis\u00a0of cholesterol was studied. It contained antipsychotic and antidepressant drugs, as well as the inhibitors of\u00a0cholesterol biosynthesis,\u00a0simvastatin, betulin, and its derivatives. All compounds were demonstrated to be cytotoxic to colon cancer cells but not to non-cancerous cells. Moreover, the most active compounds decreased the level of free cellular cholesterol. The interaction of drugs with raft-mimicking\u00a0model membranes\u00a0was visualized. All compounds reduced the size of\u00a0lipid\u00a0domains, however, only some affected their number and shape. Membrane interactions of betulin and its novel derivatives were characterized in detail.\u00a0Molecular modeling\u00a0indicated that high dipole moment and significant\u00a0lipophilicity\u00a0were characteristic for the most potent antiproliferative agents. The importance of membrane interactions of cholesterol homeostasis-affecting compounds, especially betulin derivatives, for their anticancer potency was suggested.<\/p>\n","protected":false},"featured_media":0,"template":"","products_tags":[129],"resource_type":[75],"application_areas":[53],"therapeutic_areas":[57,143],"target_categories":[],"target_families":[],"targets":[],"resource_keyword":[405,406,407,408],"class_list":["post-11391","resource_library","type-resource_library","status-publish","hentry","products_tags-vesicle-prep-pro","resource_type-publication","application_areas-assay-development-and-validation","therapeutic_areas-cancer","therapeutic_areas-assay-development-and-validation","resource_keyword-lipid-membranes","resource_keyword-membrane-bilayers","resource_keyword-cholesterol","resource_keyword-lipid-rafts"],"acf":[],"_links":{"self":[{"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/resource_library\/11391","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=11391"}],"wp:term":[{"taxonomy":"products_tags","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/products_tags?post=11391"},{"taxonomy":"resource_type","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/resource_type?post=11391"},{"taxonomy":"application_areas","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/application_areas?post=11391"},{"taxonomy":"therapeutic_areas","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/therapeutic_areas?post=11391"},{"taxonomy":"target_categories","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/target_categories?post=11391"},{"taxonomy":"target_families","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/target_families?post=11391"},{"taxonomy":"targets","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/targets?post=11391"},{"taxonomy":"resource_keyword","embeddable":true,"href":"https:\/\/nanion.com\/ja\/wp-json\/wp\/v2\/resource_keyword?post=11391"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}