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Phase I clinical, pharmacokinetic, and pharmacodynamic study of the Akt-inhibitor triciribine phosphate monohydrate in patients with advanced hematologic malignancies.在晚期血液恶性肿瘤患者中进行 Akt 抑制剂三尖杉酯碱磷酸单水合物的 I 期临床、药代动力学和药效学研究。
Leuk Res. 2013 Nov;37(11):1461-7. doi: 10.1016/j.leukres.2013.07.034. Epub 2013 Aug 6.
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Phase I pharmacokinetic and pharmacodynamic study of triciribine phosphate monohydrate, a small-molecule inhibitor of AKT phosphorylation, in adult subjects with solid tumors containing activated AKT.一水磷酸曲沙他滨的 I 期药代动力学和药效学研究，一种小分子 AKT 磷酸化抑制剂，用于含 AKT 激活的实体瘤成年患者。
Invest New Drugs. 2011 Dec;29(6):1381-9. doi: 10.1007/s10637-010-9479-2. Epub 2010 Jul 20.
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The Akt activation inhibitor TCN-P inhibits Akt phosphorylation by binding to the PH domain of Akt and blocking its recruitment to the plasma membrane. Akt 激活抑制剂 TCN-P 通过与 Akt 的 PH 结构域结合并阻止其募集到质膜上来抑制 Akt 磷酸化。
Cell Death Differ. 2010 Nov;17(11):1795-804. doi: 10.1038/cdd.2010.63. Epub 2010 May 21.
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Development and validation of LC/MS/MS method for Triciribine and its monophosphate metabolite in plasma and RBC: Application to mice pharmacokinetic studies.建立并验证 LC/MS/MS 法用于测定血浆和 RBC 中的曲昔匹特及其单磷酸代谢物：在小鼠药代动力学研究中的应用。
J Chromatogr B Analyt Technol Biomed Life Sci. 2021 Jun 1;1174:122714. doi: 10.1016/j.jchromb.2021.122714. Epub 2021 Apr 20.
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The Akt inhibitor triciribine sensitizes prostate carcinoma cells to TRAIL-induced apoptosis.Akt抑制剂曲西立滨使前列腺癌细胞对TRAIL诱导的凋亡敏感。
Int J Cancer. 2009 Aug 15;125(4):932-41. doi: 10.1002/ijc.24374.
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Phosphorylation of triciribine is necessary for activity against HIV type 1.三嗪核苷的磷酸化对于其抗1型艾滋病毒的活性是必需的。
AIDS Res Hum Retroviruses. 1998 Oct 10;14(15):1315-22. doi: 10.1089/aid.1998.14.1315.
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Proapoptotic activity and chemosensitizing effect of the novel Akt inhibitor perifosine in acute myelogenous leukemia cells.新型Akt抑制剂哌立福新在急性髓性白血病细胞中的促凋亡活性及化学增敏作用
Leukemia. 2008 Jan;22(1):147-60. doi: 10.1038/sj.leu.2404980. Epub 2007 Oct 11.
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Control of proliferation in astrocytoma cells by the receptor tyrosine kinase/PI3K/AKT signaling axis and the use of PI-103 and TCN as potential anti-astrocytoma therapies.受体酪氨酸激酶/PI3K/AKT 信号轴对星形细胞瘤细胞增殖的控制作用，以及使用 PI-103 和 TCN 作为潜在的抗星形细胞瘤治疗方法。
Neuro Oncol. 2011 Jun;13(6):610-21. doi: 10.1093/neuonc/nor035.
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SNS-032 inhibits mTORC1/mTORC2 activity in acute myeloid leukemia cells and has synergistic activity with perifosine against Akt.SNS-032 抑制急性髓系白血病细胞中的 mTORC1/mTORC2 活性，并与帕非昔布联合作用于 Akt。
J Hematol Oncol. 2013 Feb 18;6:18. doi: 10.1186/1756-8722-6-18.
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Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies.在血液系统恶性肿瘤模型中单独及联合抗癌药物对新型泛 PIM 激酶抑制剂 INCB053914 的临床前特征进行研究。
PLoS One. 2018 Jun 21;13(6):e0199108. doi: 10.1371/journal.pone.0199108. eCollection 2018.
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AKT and DUBs: a bidirectional relationship.AKT与去泛素化酶：一种双向关系。
Cell Mol Biol Lett. 2025 Jul 7;30(1):77. doi: 10.1186/s11658-025-00753-3.
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Combination of triciribine and p38 MAPK inhibitor PD169316 enhances the differentiation effect on myeloid leukemia cells.曲西立滨与p38丝裂原活化蛋白激酶抑制剂PD169316联合使用可增强对髓系白血病细胞的分化作用。
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FGTI-2734 Inhibits ERK Reactivation to Overcome Sotorasib Resistance in KRAS G12C Lung Cancer.FGTI-2734抑制ERK再激活以克服KRAS G12C肺癌中的索托拉西布耐药性。
J Thorac Oncol. 2025 Mar;20(3):331-344. doi: 10.1016/j.jtho.2024.11.022. Epub 2024 Nov 26.
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Identification of triciribine as a novel myeloid cell differentiation inducer.鉴定曲古抑菌素 A 为一种新型的髓系细胞分化诱导剂。
PLoS One. 2024 May 14;19(5):e0303428. doi: 10.1371/journal.pone.0303428. eCollection 2024.
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The Novel Link between Gene Expression Profiles of Adult T-Cell Leukemia/Lymphoma Patients' Peripheral Blood Lymphocytes and Ferroptosis Susceptibility.成人 T 细胞白血病/淋巴瘤患者外周血淋巴细胞基因表达谱与铁死亡易感性的新关联。
Genes (Basel). 2023 Oct 27;14(11):2005. doi: 10.3390/genes14112005.
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Triciribine attenuates pathological neovascularization and vascular permeability in a mouse model of proliferative retinopathy.曲昔派特抑制增生性视网膜病变小鼠模型中的病理性新生血管形成和血管通透性。
Biomed Pharmacother. 2023 Jun;162:114714. doi: 10.1016/j.biopha.2023.114714. Epub 2023 Apr 18.
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Augmenting Venetoclax Activity Through Signal Transduction in AML.通过急性髓系白血病中的信号转导增强维奈托克活性。
J Cell Signal. 2023;4(1):1-12. doi: 10.33696/signaling.4.085.
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Targeting PI3K/Akt signaling in prostate cancer therapy.在前列腺癌治疗中靶向PI3K/Akt信号通路
J Cell Commun Signal. 2023 Sep;17(3):423-443. doi: 10.1007/s12079-022-00702-1. Epub 2022 Nov 11.
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Targeting PI3K/Akt signal transduction for cancer therapy.针对 PI3K/Akt 信号转导通路的癌症治疗策略。
Signal Transduct Target Ther. 2021 Dec 16;6(1):425. doi: 10.1038/s41392-021-00828-5.
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Akt isoforms differentially provide for chemoresistance in prostate cancer.Akt亚型在前列腺癌中对化疗耐药性的作用存在差异。
Cancer Biol Med. 2021 Oct 1;19(5):635-50. doi: 10.20892/j.issn.2095-3941.2020.0747.
本文引用的文献
1
AKT inhibition by triciribine alone or as combination therapy for growth control of gastroenteropancreatic neuroendocrine tumors.曲昔匹特单独或联合治疗抑制 AKT 用于控制胃肠胰神经内分泌肿瘤的生长。
Int J Oncol. 2012 Mar;40(3):876-88. doi: 10.3892/ijo.2011.1256. Epub 2011 Nov 7.
2
Combination of farnesyltransferase and Akt inhibitors is synergistic in breast cancer cells and causes significant breast tumor regression in ErbB2 transgenic mice.法尼基转移酶和 Akt 抑制剂联合使用在乳腺癌细胞中具有协同作用，并导致 ErbB2 转基因小鼠的乳腺肿瘤显著消退。
Clin Cancer Res. 2011 May 1;17(9):2852-62. doi: 10.1158/1078-0432.CCR-10-2544.
3
A phase I/II study of imatinib plus reinduction therapy for c-kit-positive relapsed/refractory acute myeloid leukemia: inhibition of Akt activation correlates with complete response.一项伊马替尼联合再诱导治疗 c-kit 阳性复发/难治性急性髓系白血病的 I/II 期研究： Akt 激活的抑制与完全缓解相关。
Leukemia. 2011 Jun;25(6):945-52. doi: 10.1038/leu.2011.34. Epub 2011 Mar 15.
4
Acute myeloid leukemia.急性髓系白血病
J Natl Compr Canc Netw. 2011 Mar;9(3):280-317. doi: 10.6004/jnccn.2011.0027.
5
Therapeutic advances in acute myeloid leukemia.急性髓细胞白血病的治疗进展。
J Clin Oncol. 2011 Feb 10;29(5):487-94. doi: 10.1200/JCO.2010.30.1820. Epub 2011 Jan 10.
6
Preclinical testing of the Akt inhibitor triciribine in T-cell acute lymphoblastic leukemia.在 T 细胞急性淋巴细胞白血病中 Akt 抑制剂曲昔派特的临床前试验。
J Cell Physiol. 2011 Mar;226(3):822-31. doi: 10.1002/jcp.22407.
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FLT3 inhibitors for the treatment of acute myeloid leukemia.用于治疗急性髓系白血病的FLT3抑制剂
Clin Adv Hematol Oncol. 2010 Jun;8(6):429-36, 444.
8
Phase I pharmacokinetic and pharmacodynamic study of triciribine phosphate monohydrate, a small-molecule inhibitor of AKT phosphorylation, in adult subjects with solid tumors containing activated AKT.一水磷酸曲沙他滨的 I 期药代动力学和药效学研究，一种小分子 AKT 磷酸化抑制剂，用于含 AKT 激活的实体瘤成年患者。
Invest New Drugs. 2011 Dec;29(6):1381-9. doi: 10.1007/s10637-010-9479-2. Epub 2010 Jul 20.
9
The Akt activation inhibitor TCN-P inhibits Akt phosphorylation by binding to the PH domain of Akt and blocking its recruitment to the plasma membrane. Akt 激活抑制剂 TCN-P 通过与 Akt 的 PH 结构域结合并阻止其募集到质膜上来抑制 Akt 磷酸化。
Cell Death Differ. 2010 Nov;17(11):1795-804. doi: 10.1038/cdd.2010.63. Epub 2010 May 21.
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Receptor tyrosine kinase alterations in AML - biology and therapy.急性髓系白血病中的受体酪氨酸激酶改变——生物学与治疗
Cancer Treat Res. 2010;145:85-108. doi: 10.1007/978-0-387-69259-3_6.
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