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Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma

Ioanna Papandreou, Nicholas C Denko, Michael Olson, Heleen Van Melckebeke UGent, Sofie Lust UGent, Arvin Tam, David E Solow-Cordero, Donna M Bouley, Fritz Offner UGent and Maho Niwa, et al. (2011) BLOOD. 117(4). p.1311-1314
abstract
Activation of the adaptive Ire1-XBP1 pathway has been identified in many solid tumors and hematologic malignancies, including multiple myeloma (MM). Here, we report the identification of STF-083010, a novel small-molecule inhibitor of Ire1. STF-083010 inhibited Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress both in vitro and in vivo. Treatment with STF-083010 showed significant antimy-eloma activity in model human MM xenografts. Similarly, STF-083010 was preferentially toxic to freshly isolated human CD138(+) MM cells compared with other similarly isolated cell populations. The identification of this novel Ire1 inhibitor supports the hypothesis that the Ire1-XBP1 axis is a promising target for anticancer therapy, especially in the context of MM.
Please use this url to cite or link to this publication:
author
organization
year
type
journalArticle (original)
publication status
published
subject
keyword
KINASE/ENDORIBONUCLEASE IRE1P, UNFOLDED PROTEIN RESPONSE, TUMOR-GROWTH, ACTIVATION, CELLS, REVEALS, PATHWAY
journal title
BLOOD
Blood
volume
117
issue
4
pages
1311 - 1314
Web of Science type
Article
Web of Science id
000286623400029
JCR category
HEMATOLOGY
JCR impact factor
9.898 (2011)
JCR rank
2/68 (2011)
JCR quartile
1 (2011)
ISSN
0006-4971
DOI
10.1182/blood-2010-08-303099
language
English
UGent publication?
yes
classification
A1
copyright statement
I have transferred the copyright for this publication to the publisher
id
2005652
handle
http://hdl.handle.net/1854/LU-2005652
date created
2012-01-27 10:20:38
date last changed
2012-02-14 17:36:58
@article{2005652,
  abstract     = {Activation of the adaptive Ire1-XBP1 pathway has been identified in many solid tumors and hematologic malignancies, including multiple myeloma (MM). Here, we report the identification of STF-083010, a novel small-molecule inhibitor of Ire1. STF-083010 inhibited Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress both in vitro and in vivo. Treatment with STF-083010 showed significant antimy-eloma activity in model human MM xenografts. Similarly, STF-083010 was preferentially toxic to freshly isolated human CD138(+) MM cells compared with other similarly isolated cell populations. The identification of this novel Ire1 inhibitor supports the hypothesis that the Ire1-XBP1 axis is a promising target for anticancer therapy, especially in the context of MM.},
  author       = {Papandreou, Ioanna and Denko, Nicholas C and Olson, Michael and Van Melckebeke, Heleen and Lust, Sofie and Tam, Arvin and Solow-Cordero, David E and Bouley, Donna M and Offner, Fritz and Niwa, Maho and Koong, Albert C},
  issn         = {0006-4971},
  journal      = {BLOOD},
  keyword      = {KINASE/ENDORIBONUCLEASE IRE1P,UNFOLDED PROTEIN RESPONSE,TUMOR-GROWTH,ACTIVATION,CELLS,REVEALS,PATHWAY},
  language     = {eng},
  number       = {4},
  pages        = {1311--1314},
  title        = {Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma},
  url          = {http://dx.doi.org/10.1182/blood-2010-08-303099},
  volume       = {117},
  year         = {2011},
}

Chicago
Papandreou, Ioanna, Nicholas C Denko, Michael Olson, Heleen Van Melckebeke, SOFIE LUST, Arvin Tam, David E Solow-Cordero, et al. 2011. “Identification of an Ire1alpha Endonuclease Specific Inhibitor with Cytotoxic Activity Against Human Multiple Myeloma.” Blood 117 (4): 1311–1314.
APA
Papandreou, I., Denko, N. C., Olson, M., Van Melckebeke, H., LUST, S., Tam, A., Solow-Cordero, D. E., et al. (2011). Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma. BLOOD, 117(4), 1311–1314.
Vancouver
1.
Papandreou I, Denko NC, Olson M, Van Melckebeke H, LUST S, Tam A, et al. Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma. BLOOD. 2011;117(4):1311–4.
MLA
Papandreou, Ioanna, Nicholas C Denko, Michael Olson, et al. “Identification of an Ire1alpha Endonuclease Specific Inhibitor with Cytotoxic Activity Against Human Multiple Myeloma.” BLOOD 117.4 (2011): 1311–1314. Print.