The PI3K/Akt/mTOR signaling pathway is one of the most frequently dysregulated pathways in cancer.Targeting the PI3K-mediated pathway has been an important strategy for developing novel anticancer agents.In the past d...The PI3K/Akt/mTOR signaling pathway is one of the most frequently dysregulated pathways in cancer.Targeting the PI3K-mediated pathway has been an important strategy for developing novel anticancer agents.In the past decades,more than 40 inhibitors of the PI3K/Akt/mTOR pathway have been developed at different clinical stages.Temsirolimus,everolimus,idelalisib,and copanlisib have been approved for clinical use by the Food and Drug Administration of the United States(FDA).However,the toxic-ity and drug resistance limit their efficiency in the treatment.Novel compounds with greater potency and selectivity,as well as im-proved therapeutic indices with reduced toxicity,are clearly required.Over the past three decades,a lot of bioactive ingredients with anticancer effects by affecting the PI3K-mediated pathways have been found from marine organisms.In the present mini-review,anticancer compounds from marine source that target the PI3K/Akt/mTOR signaling were reviewed.The molecular entities and their modes of action were presented.The marine compounds targeting special factors of the PI3K/Akt/mTOR were highlighted.展开更多
基金The study was supported by the National Natural Sci-ence Foundation of China(Nos.81573457 and 81773776)We are also grateful to the support from the Taishan Talents Project of Shandong Province and the Department of Science and Technology in Shandong Province of China(Nos.ZR2017MH117,2018YYSP025,and ZR2017MH 027)Department of Science and Technology of Si-chuan Province,China(Nos.2017HH0104 and 2019YFS 0116).
文摘The PI3K/Akt/mTOR signaling pathway is one of the most frequently dysregulated pathways in cancer.Targeting the PI3K-mediated pathway has been an important strategy for developing novel anticancer agents.In the past decades,more than 40 inhibitors of the PI3K/Akt/mTOR pathway have been developed at different clinical stages.Temsirolimus,everolimus,idelalisib,and copanlisib have been approved for clinical use by the Food and Drug Administration of the United States(FDA).However,the toxic-ity and drug resistance limit their efficiency in the treatment.Novel compounds with greater potency and selectivity,as well as im-proved therapeutic indices with reduced toxicity,are clearly required.Over the past three decades,a lot of bioactive ingredients with anticancer effects by affecting the PI3K-mediated pathways have been found from marine organisms.In the present mini-review,anticancer compounds from marine source that target the PI3K/Akt/mTOR signaling were reviewed.The molecular entities and their modes of action were presented.The marine compounds targeting special factors of the PI3K/Akt/mTOR were highlighted.