Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics
Mustapha Haddach
1
,
Michael K Schwaebe
1
,
Jerome Michaux
1
,
Johnny Nagasawa
1
,
Sean E O'Brien
1
,
Jeffrey P Whitten
1
,
Fabrice Pierre
1
,
Pauline Kerdoncuff
1
,
Levan Darjania
1
,
Ryan Stansfield
1
,
Denis Drygin
1
,
Kenna Anderes
1
,
Chris Proffitt
1
,
Josh Bliesath
1
,
Adam Siddiqui-Jain
1
,
May Omori
1
,
Nanni Huser
1
,
William G Rice
1
,
David M. Ryckman
1
1
Cylene Pharmaceuticals, 5820
Nancy Ridge Drive, Suite 200, San Diego, California 92121, United
States
|
Publication type: Journal Article
Publication date: 2012-06-08
scimago Q1
wos Q2
SJR: 0.805
CiteScore: 5.8
Impact factor: 4.0
ISSN: 19485875
PubMed ID:
24900516
Organic Chemistry
Drug Discovery
Biochemistry
Abstract
Accelerated proliferation of solid tumor and hematologic cancer cells is linked to accelerated transcription of rDNA by the RNA polymerase I (Pol I) enzyme to produce elevated levels of rRNA (rRNA). Indeed, upregulation of Pol I, frequently caused by mutational alterations among tumor suppressors and oncogenes, is required for maintenance of the cancer phenotype and forms the basis for seeking selective inhibitors of Pol I as anticancer therapeutics. 2-(4-Methyl-[1,4]diazepan-1-yl)-5-oxo-5H-7-thia-1,11b-diaza-benzo[c]fluorene-6-carboxylic acid (5-methyl-pyrazin-2-ylmethyl)-amide (CX-5461, 7c) has been identified as the first potent, selective, and orally bioavailable inhibitor of RNA Pol I transcription with in vivo activity in tumor growth efficacy models. The preclinical data support the development of CX-5461 as an anticancer drug with potential for activity in several types of cancer.
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Metrics
140
Total citations:
140
Citations from 2024:
32
(22.86%)
Cite this
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MLA
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GOST
Copy
Haddach M. et al. Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics // ACS Medicinal Chemistry Letters. 2012. Vol. 3. No. 7. pp. 602-606.
GOST all authors (up to 50)
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Haddach M., Schwaebe M. K., Michaux J., Nagasawa J., O'Brien S. E., Whitten J. P., Pierre F., Kerdoncuff P., Darjania L., Stansfield R., Drygin D., Anderes K., Proffitt C., Bliesath J., Siddiqui-Jain A., Omori M., Huser N., Rice W. G., Ryckman D. M. Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics // ACS Medicinal Chemistry Letters. 2012. Vol. 3. No. 7. pp. 602-606.
Cite this
RIS
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TY - JOUR
DO - 10.1021/ml300110s
UR - https://doi.org/10.1021/ml300110s
TI - Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics
T2 - ACS Medicinal Chemistry Letters
AU - Haddach, Mustapha
AU - Schwaebe, Michael K
AU - Michaux, Jerome
AU - Nagasawa, Johnny
AU - O'Brien, Sean E
AU - Whitten, Jeffrey P
AU - Pierre, Fabrice
AU - Kerdoncuff, Pauline
AU - Darjania, Levan
AU - Stansfield, Ryan
AU - Drygin, Denis
AU - Anderes, Kenna
AU - Proffitt, Chris
AU - Bliesath, Josh
AU - Siddiqui-Jain, Adam
AU - Omori, May
AU - Huser, Nanni
AU - Rice, William G
AU - Ryckman, David M.
PY - 2012
DA - 2012/06/08
PB - American Chemical Society (ACS)
SP - 602-606
IS - 7
VL - 3
PMID - 24900516
SN - 1948-5875
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2012_Haddach,
author = {Mustapha Haddach and Michael K Schwaebe and Jerome Michaux and Johnny Nagasawa and Sean E O'Brien and Jeffrey P Whitten and Fabrice Pierre and Pauline Kerdoncuff and Levan Darjania and Ryan Stansfield and Denis Drygin and Kenna Anderes and Chris Proffitt and Josh Bliesath and Adam Siddiqui-Jain and May Omori and Nanni Huser and William G Rice and David M. Ryckman},
title = {Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics},
journal = {ACS Medicinal Chemistry Letters},
year = {2012},
volume = {3},
publisher = {American Chemical Society (ACS)},
month = {jun},
url = {https://doi.org/10.1021/ml300110s},
number = {7},
pages = {602--606},
doi = {10.1021/ml300110s}
}
Cite this
MLA
Copy
Haddach, Mustapha, et al. “Discovery of CX-5461, the First Direct and Selective Inhibitor of RNA Polymerase I, for Cancer Therapeutics.” ACS Medicinal Chemistry Letters, vol. 3, no. 7, Jun. 2012, pp. 602-606. https://doi.org/10.1021/ml300110s.