Nuclear Imaging Study of the Pharmacodynamic Effects of Debio 1143, an Antagonist of Multiple Inhibitor of Apoptosis Proteins (IAPs), in a Triple-Negative Breast Cancer Model
Joint Authors
Oudot, Alexandra
Vrigneaud, Jean-Marc
Denat, Franck
Bellaye, Pierre-Simon
Raguin, Olivier
Bichat, Francis
Vaslin, Anne
Maby-El Hajjami, Hélène
Zanna, Claudio
Vuagniaux, Grégoire
Fumoleau, Pierre
Brunotte, François
Collin, Bertrand
Source
Contrast Media & Molecular Imaging
Issue
Vol. 2018, Issue 2018 (31 Dec. 2018), pp.1-11, 11 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2018-12-02
Country of Publication
Egypt
No. of Pages
11
Main Subjects
Abstract EN
Background.
Debio 1143, a potent orally available SMAC mimetic, targets inhibitors of apoptosis proteins (IAPs) members and is currently in clinical trials.
In this study, nuclear imaging evaluated the effects of Debio 1143 on tumor cell death and metabolism in a triple-negative breast cancer (TNBC) cell line (MDA-MB-231)-based animal model.
Methods.
Apoptosis induced by Debio 1143 was assessed by FACS (caspase-3, annexin 5 (A5)), binding of 99mTc-HYNIC-Annexin V, and a cell proliferation assay.
99mTc-HYNIC-Annexin V SPECT and [18F]-FDG PET were also performed in mice xenografted with MDA-MB-231 cells.
Results.
Debio 1143 induced early apoptosis both in vitro and in vivo 6 h after treatment.
Debio 1143 inhibited tumor growth, which was associated with a decreased tumor [18F]-FDG uptake when measured during treatment.
Conclusions.
This imaging study combining SPECT and PET showed the early proapoptotic effects of Debio 1143 resulting in a robust antitumor activity in a preclinical TNBC model.
These imaging biomarkers represent valuable noninvasive tools for translational and clinical research in TNBC.
American Psychological Association (APA)
Bellaye, Pierre-Simon& Oudot, Alexandra& Vrigneaud, Jean-Marc& Raguin, Olivier& Bichat, Francis& Vaslin, Anne…[et al.]. 2018. Nuclear Imaging Study of the Pharmacodynamic Effects of Debio 1143, an Antagonist of Multiple Inhibitor of Apoptosis Proteins (IAPs), in a Triple-Negative Breast Cancer Model. Contrast Media & Molecular Imaging،Vol. 2018, no. 2018, pp.1-11.
https://search.emarefa.net/detail/BIM-1131590
Modern Language Association (MLA)
Bellaye, Pierre-Simon…[et al.]. Nuclear Imaging Study of the Pharmacodynamic Effects of Debio 1143, an Antagonist of Multiple Inhibitor of Apoptosis Proteins (IAPs), in a Triple-Negative Breast Cancer Model. Contrast Media & Molecular Imaging No. 2018 (2018), pp.1-11.
https://search.emarefa.net/detail/BIM-1131590
American Medical Association (AMA)
Bellaye, Pierre-Simon& Oudot, Alexandra& Vrigneaud, Jean-Marc& Raguin, Olivier& Bichat, Francis& Vaslin, Anne…[et al.]. Nuclear Imaging Study of the Pharmacodynamic Effects of Debio 1143, an Antagonist of Multiple Inhibitor of Apoptosis Proteins (IAPs), in a Triple-Negative Breast Cancer Model. Contrast Media & Molecular Imaging. 2018. Vol. 2018, no. 2018, pp.1-11.
https://search.emarefa.net/detail/BIM-1131590
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1131590