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本文引用的文献

1
Biomarker and pharmacologic evaluation of the γ-secretase inhibitor PF-03084014 in breast cancer models.γ-分泌酶抑制剂 PF-03084014 在乳腺癌模型中的生物标志物和药理学评价。
Clin Cancer Res. 2012 Sep 15;18(18):5008-19. doi: 10.1158/1078-0432.CCR-12-1379. Epub 2012 Jul 17.
2
Targeting the Notch pathway: twists and turns on the road to rational therapeutics.靶向Notch信号通路：通往合理治疗之路的曲折历程
J Clin Oncol. 2012 Jul 1;30(19):2418-20. doi: 10.1200/JCO.2012.42.0992. Epub 2012 May 14.
3
Preclinical analysis of the γ-secretase inhibitor PF-03084014 in combination with glucocorticoids in T-cell acute lymphoblastic leukemia.γ-分泌酶抑制剂 PF-03084014 联合糖皮质激素在 T 细胞急性淋巴细胞白血病中的临床前分析。
Mol Cancer Ther. 2012 Jul;11(7):1565-75. doi: 10.1158/1535-7163.MCT-11-0938. Epub 2012 Apr 13.
4
The double-edged sword of Notch signaling in cancer. Notch 信号通路在癌症中的双刃剑作用。
Semin Cell Dev Biol. 2012 Jun;23(4):458-64. doi: 10.1016/j.semcdb.2012.01.017. Epub 2012 Jan 30.
5
Initial testing (stage 1) by the pediatric preclinical testing program of RO4929097, a γ-secretase inhibitor targeting notch signaling.RO4929097 是一种针对 Notch 信号的 γ-分泌酶抑制剂，儿科临床前测试计划进行了初步测试（第 1 阶段）。
Pediatr Blood Cancer. 2012 May;58(5):815-8. doi: 10.1002/pbc.23290. Epub 2011 Aug 16.
6
Gamma-secretase inhibitor treatment promotes VEGF-A-driven blood vessel growth and vascular leakage but disrupts neovascular perfusion.γ-分泌酶抑制剂治疗促进 VEGF-A 驱动的血管生长和血管渗漏，但破坏新血管灌注。
PLoS One. 2011 Apr 14;6(4):e18709. doi: 10.1371/journal.pone.0018709.
7
Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: discovery of PF-3084014.新型四氢萘氨基咪唑类γ-分泌酶抑制剂的设计、合成及体内评价：PF-3084014 的发现。
Bioorg Med Chem Lett. 2011 May 1;21(9):2637-40. doi: 10.1016/j.bmcl.2010.12.118. Epub 2010 Dec 30.
8
Notch pathway inhibition significantly reduces rhabdomyosarcoma invasiveness and mobility in vitro.Notch 通路抑制显著降低横纹肌肉瘤的体外侵袭性和迁移能力。
Clin Cancer Res. 2011 Feb 1;17(3):505-13. doi: 10.1158/1078-0432.CCR-10-0166. Epub 2010 Dec 21.
9
Inhibition of notch signaling blocks growth of glioblastoma cell lines and tumor neurospheres.Notch信号通路的抑制可阻断胶质母细胞瘤细胞系和肿瘤神经球的生长。
Genes Cancer. 2010 Aug;1(8):822-35. doi: 10.1177/1947601910383564.
10
Notch signalling in T-cell lymphoblastic leukaemia/lymphoma and other haematological malignancies.Notch 信号通路在 T 细胞淋巴母细胞白血病/淋巴瘤和其他血液系统恶性肿瘤中的作用。
J Pathol. 2011 Jan;223(2):262-73. doi: 10.1002/path.2789. Epub 2010 Oct 21.

儿科临床前测试计划对 Notch 抑制剂 PF-03084014 进行初步测试（第 1 阶段）。

Initial testing (stage 1) of the notch inhibitor PF-03084014, by the pediatric preclinical testing program.

机构信息

Children's Cancer Institute Australia for Medical Research, Randwick, NSW, Australia.

出版信息

Pediatr Blood Cancer. 2014 Aug;61(8):1493-6. doi: 10.1002/pbc.25026. Epub 2014 Mar 24.

DOI:10.1002/pbc.25026
PMID:24664981
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4225044/
Abstract

PF-03084014, a γ-secretase inhibitor, was tested against the PPTP in vitro cell line panel (1.0 nM to 10 μM) and against the in vivo xenograft panels (administered orally twice daily on Days 1-7 and 15-21). PF-03084014 demonstrated limited in vitro activity, with no cell line achieving ≥50% inhibition. PF-03084014 induced significant differences in EFS distribution in 14 of 35 (40%) solid tumor xenografts, and 1 of 9 ALL xenografts (which lacked a NOTCH1 mutation), but objective responses were not observed. PF-03084014 demonstrated limited single agent activity in vitro and in vivo against the pediatric preclinical models studied.

摘要

PF-03084014，一种γ-分泌酶抑制剂，在体外细胞系（1.0 nM 至 10 μM）和体内异种移植（每天口服两次，第 1-7 天和第 15-21 天）中进行了测试。PF-03084014在体外表现出有限的活性，没有一个细胞系的抑制率达到≥50%。PF-03084014在 35 个实体瘤异种移植中的 14 个（40%）和 9 个 ALL 异种移植中的 1 个（没有 NOTCH1 突变）中诱导了 EFS 分布的显著差异，但未观察到客观反应。PF-03084014在体外和体内对所研究的儿科临床前模型表现出有限的单药活性。