A fluorescent biomarker of the polyamine transport system to select patients with AML for F14512 treatment

被引：27

作者：

Annereau, J. -P. ^{[1
]}

Brel, V. ^{[1
]}

Dumontet, C. ^{[4
]}

Guminski, Y. ^{[3
]}

Imbert, T. ^{[3
]}

Broussas, M. ^{[2
]}

Vispe, S. ^{[1
]}

Breand, S. ^{[5
]}

Guilbaud, N. ^{[1
]}

Barret, J-M. ^{[1
]}

Bailly, C. ^{[1
]}

机构：

[1] Inst Rech Pierre Fabre, Ctr Rech Oncol Expt, F-31432 Toulouse 4, France

[2] Inst Rech Pierre Fabre, Ctr Immunol Pierre Fabre, St Julien En Genevois, France

[3] Ctr Rech Pierre Fabre, Div Chim Med, F-81106 Castres, France

[4] Univ Lyon 1, INSERM, U590, F-69365 Lyon, France

[5] Ctr Rech Pierre Fabre, Serv Informat Rech, F-81106 Castres, France

来源：

LEUKEMIA RESEARCH | 2010年 / 34卷 / 10期

关键词：

F14512; Etoposide; Biomarker; Polyamine transporter; Spermine; ETOPOSIDE; ANALOGS; CELLS; BIOSYNTHESIS; DERIVATIVES; PROBE; ACID;

D O I：

10.1016/j.leukres.2009.12.021

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

The polyamine transport system (PTS), hyperactive in cancer cells, can constitute a gate to deliver F14512, a novel spermine epipodophyllotoxin conjugate recently selected for clinical development in AML phase I. We investigated in vitro the high antiproliferative effect of F14512 against 13 leukemia cell lines, and demonstrated a statistically significant correlation with the level of PTS activity, using a novel fluorescent marker F96982. This labelling protocol was then adapted for clinical applications for blood, bone marrow and AML samples with CD45 gating. Within the patient samples, the PTS activity varied significantly in AML cells, as compared to normal lymphocytes. In conclusion, the identification of PTS-positive AML with F98982 probe offers new perspectives to select patients prone to respond to F14512. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：1383 / 1389

页数：7

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