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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.
7
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.
10
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.

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。

Phase I clinical, pharmacokinetic, and pharmacodynamic study of the Akt-inhibitor triciribine phosphate monohydrate in patients with advanced hematologic malignancies.

机构信息

Departments of Experimental Therapeutics, M.D. Anderson Cancer Center, Houston, TX, USA.

出版信息

Leuk Res. 2013 Nov;37(11):1461-7. doi: 10.1016/j.leukres.2013.07.034. Epub 2013 Aug 6.

DOI:10.1016/j.leukres.2013.07.034
PMID:23993427
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4205589/
Abstract

Akt, a serine/threonine protein kinase, is constitutively phosphorylated and hyperactivated in multiple cancers, including acute myeloid leukemia. High levels are linked to poor survival and inferior responses to chemotherapy, making Akt inhibition an attractive therapeutic target. In this phase I/II study of TCN-PM, a small-molecule Akt inhibitor, TCN-PM therapy was well tolerated in patients with advanced hematological malignancies, and reduced levels of phosphorylation of Akt and its substrate Bad were shown, consistent with inhibition of this survival pathway and induction of cell death. Further investigation of TCN-PM alone or in combination in patients with high Akt levels is warranted.

摘要

Akt 是一种丝氨酸/苏氨酸蛋白激酶，在多种癌症中持续磷酸化和过度激活，包括急性髓性白血病。高水平与不良生存和对化疗反应不良相关，使得 Akt 抑制成为一个有吸引力的治疗靶点。在这项 TCN-PM（一种小分子 Akt 抑制剂）的 I/II 期研究中，TCN-PM 治疗在晚期血液恶性肿瘤患者中耐受性良好，并且显示 Akt 和其底物 Bad 的磷酸化水平降低，与该存活途径的抑制和细胞死亡的诱导一致。进一步研究 TCN-PM 单独或联合用于高 Akt 水平的患者是合理的。