{"title":"从天然产物PHGDH抑制剂研究的见解","authors":"Zhaodan Wang, Xueqin Chen, Qingxiang Sun","doi":"10.33696/signaling.3.073","DOIUrl":null,"url":null,"abstract":"The synthetic activity of serine is significantly upregulated in several cancers [1]. Homo sapiens 3-phosphoglycerate dehydrogenase (PHGDH) catalyzes the rate-limiting step of serine synthesis, which converts 3-phosphoglycerate (3PG) and NAD+ to 3-phosphohydroxypyruvate and NADH [2,3]. PHGDH inhibitors were extensively pursued recently for their use in the treatment of affected cancers [4,5]. Among the inhibitors identified, three natural products including azacoccone E [6], ixocarpalactone A [7], withaferin A and oridonin [8] were shown to effectively inhibit PHGDH enzyme activity and cancer cell growth.","PeriodicalId":73645,"journal":{"name":"Journal of cellular signaling","volume":"92 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2022-06-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Insights from Natural Product PHGDH Inhibitor Studies\",\"authors\":\"Zhaodan Wang, Xueqin Chen, Qingxiang Sun\",\"doi\":\"10.33696/signaling.3.073\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The synthetic activity of serine is significantly upregulated in several cancers [1]. Homo sapiens 3-phosphoglycerate dehydrogenase (PHGDH) catalyzes the rate-limiting step of serine synthesis, which converts 3-phosphoglycerate (3PG) and NAD+ to 3-phosphohydroxypyruvate and NADH [2,3]. PHGDH inhibitors were extensively pursued recently for their use in the treatment of affected cancers [4,5]. Among the inhibitors identified, three natural products including azacoccone E [6], ixocarpalactone A [7], withaferin A and oridonin [8] were shown to effectively inhibit PHGDH enzyme activity and cancer cell growth.\",\"PeriodicalId\":73645,\"journal\":{\"name\":\"Journal of cellular signaling\",\"volume\":\"92 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2022-06-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of cellular signaling\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.33696/signaling.3.073\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of cellular signaling","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.33696/signaling.3.073","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Insights from Natural Product PHGDH Inhibitor Studies
The synthetic activity of serine is significantly upregulated in several cancers [1]. Homo sapiens 3-phosphoglycerate dehydrogenase (PHGDH) catalyzes the rate-limiting step of serine synthesis, which converts 3-phosphoglycerate (3PG) and NAD+ to 3-phosphohydroxypyruvate and NADH [2,3]. PHGDH inhibitors were extensively pursued recently for their use in the treatment of affected cancers [4,5]. Among the inhibitors identified, three natural products including azacoccone E [6], ixocarpalactone A [7], withaferin A and oridonin [8] were shown to effectively inhibit PHGDH enzyme activity and cancer cell growth.