{"title":"强效 Ca2+ ATP 酶抑制剂 Iezoside 的结构-活性关系研究","authors":"Naoaki Kurisawa, Kazuya Teranuma, Akari Noto, Arihiro Iwasaki, Yoshiki Kabashima, Rie Nakajima, Chikashi Toyoshima, Kiyotake Suenaga","doi":"10.1093/bulcsj/uoae070","DOIUrl":null,"url":null,"abstract":"Iezoside (1a) is a novel, potent sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) inhibitor from marine cyanobacterium. This paper describes the synthesis of comprehensive iezoside (1a) analogs containing C18/19 diastereomers, simplified analogs without the peptide unit, and aglycones. Evaluations of the antiproliferative activities against cancer cells and SERCA inhibitory activities of the synthesized analogs revealed how the absolute configurations at C18/19, peptide, and the sugar unit contribute to each bioactivity.Ca2+ ATPase (SERCA) inhibitor, Structure-activity relationship, Marine natural products","PeriodicalId":9511,"journal":{"name":"Bulletin of the Chemical Society of Japan","volume":"64 1","pages":""},"PeriodicalIF":3.3000,"publicationDate":"2024-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Structure-Activity Relationship Studies on Iezoside, a Highly Potent Ca2+ ATPase Inhibitor\",\"authors\":\"Naoaki Kurisawa, Kazuya Teranuma, Akari Noto, Arihiro Iwasaki, Yoshiki Kabashima, Rie Nakajima, Chikashi Toyoshima, Kiyotake Suenaga\",\"doi\":\"10.1093/bulcsj/uoae070\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Iezoside (1a) is a novel, potent sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) inhibitor from marine cyanobacterium. This paper describes the synthesis of comprehensive iezoside (1a) analogs containing C18/19 diastereomers, simplified analogs without the peptide unit, and aglycones. Evaluations of the antiproliferative activities against cancer cells and SERCA inhibitory activities of the synthesized analogs revealed how the absolute configurations at C18/19, peptide, and the sugar unit contribute to each bioactivity.Ca2+ ATPase (SERCA) inhibitor, Structure-activity relationship, Marine natural products\",\"PeriodicalId\":9511,\"journal\":{\"name\":\"Bulletin of the Chemical Society of Japan\",\"volume\":\"64 1\",\"pages\":\"\"},\"PeriodicalIF\":3.3000,\"publicationDate\":\"2024-07-06\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Bulletin of the Chemical Society of Japan\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://doi.org/10.1093/bulcsj/uoae070\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Bulletin of the Chemical Society of Japan","FirstCategoryId":"92","ListUrlMain":"https://doi.org/10.1093/bulcsj/uoae070","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Structure-Activity Relationship Studies on Iezoside, a Highly Potent Ca2+ ATPase Inhibitor
Iezoside (1a) is a novel, potent sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) inhibitor from marine cyanobacterium. This paper describes the synthesis of comprehensive iezoside (1a) analogs containing C18/19 diastereomers, simplified analogs without the peptide unit, and aglycones. Evaluations of the antiproliferative activities against cancer cells and SERCA inhibitory activities of the synthesized analogs revealed how the absolute configurations at C18/19, peptide, and the sugar unit contribute to each bioactivity.Ca2+ ATPase (SERCA) inhibitor, Structure-activity relationship, Marine natural products
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The Bulletin of the Chemical Society of Japan (BCSJ) is devoted to the publication of scientific research papers in the fields of Theoretical and Physical Chemistry, Analytical and Inorganic Chemistry, Organic and Biological Chemistry, and Applied and Materials Chemistry. BCSJ appears as a monthly journal online and in advance with three kinds of papers (Accounts, Articles, and Short Articles) describing original research. The purpose of BCSJ is to select and publish the most important papers with the broadest significance to the chemistry community in general. The Chemical Society of Japan hopes all visitors will notice the usefulness of our journal and the abundance of topics, and welcomes more submissions from scientists all over the world.
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