ACS Medicinal Chemistry Letters, volume 3, issue 7, pages 602-606
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
Journal:
ACS Medicinal Chemistry Letters
Quartile SCImago
Q1
Quartile WOS
Q2
Impact factor: 4.2
ISSN: 19485875, 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.
Top-30
Journals
|
1
2
3
4
5
|
|
|
International Journal of Molecular Sciences
5 publications, 4.13%
|
|
|
Cancers
5 publications, 4.13%
|
|
|
Biomedicines
4 publications, 3.31%
|
|
|
Scientific Reports
3 publications, 2.48%
|
|
|
Journal of Biological Chemistry
3 publications, 2.48%
|
|
|
eLife
3 publications, 2.48%
|
|
|
Oncotarget
2 publications, 1.65%
|
|
|
Cells
2 publications, 1.65%
|
|
|
Genes
2 publications, 1.65%
|
|
|
Investigational New Drugs
2 publications, 1.65%
|
|
|
Journal of Controlled Release
2 publications, 1.65%
|
|
|
PLoS ONE
2 publications, 1.65%
|
|
|
Biochimica et Biophysica Acta - Gene Regulatory Mechanisms
2 publications, 1.65%
|
|
|
European Journal of Medicinal Chemistry
2 publications, 1.65%
|
|
|
Chemistry - A European Journal
2 publications, 1.65%
|
|
|
Nucleic Acids Research
2 publications, 1.65%
|
|
|
Cancer Research
2 publications, 1.65%
|
|
|
Australian Journal of Chemistry
1 publication, 0.83%
|
|
|
International Journal of Hematology
1 publication, 0.83%
|
|
|
Arteriosclerosis, Thrombosis, and Vascular Biology
1 publication, 0.83%
|
|
|
Transplantation
1 publication, 0.83%
|
|
|
Molecules
1 publication, 0.83%
|
|
|
Pharmaceuticals
1 publication, 0.83%
|
|
|
Frontiers in Chemistry
1 publication, 0.83%
|
|
|
Frontiers in Pharmacology
1 publication, 0.83%
|
|
|
Cellular and Molecular Life Sciences
1 publication, 0.83%
|
|
|
Signal Transduction and Targeted Therapy
1 publication, 0.83%
|
|
|
Nature Communications
1 publication, 0.83%
|
|
|
Laboratory Investigation
1 publication, 0.83%
|
|
|
1
2
3
4
5
|
Publishers
|
5
10
15
20
25
|
|
|
Elsevier
24 publications, 19.83%
|
|
|
MDPI
20 publications, 16.53%
|
|
|
Springer Nature
16 publications, 13.22%
|
|
|
Cold Spring Harbor Laboratory
10 publications, 8.26%
|
|
|
American Chemical Society (ACS)
6 publications, 4.96%
|
|
|
American Association for Cancer Research (AACR)
5 publications, 4.13%
|
|
|
Wiley
4 publications, 3.31%
|
|
|
Oxford University Press
4 publications, 3.31%
|
|
|
Frontiers Media S.A.
3 publications, 2.48%
|
|
|
American Society for Biochemistry and Molecular Biology
3 publications, 2.48%
|
|
|
Public Library of Science (PLoS)
3 publications, 2.48%
|
|
|
Royal Society of Chemistry (RSC)
3 publications, 2.48%
|
|
|
eLife Sciences Publications
3 publications, 2.48%
|
|
|
Impact Journals
2 publications, 1.65%
|
|
|
Ovid Technologies (Wolters Kluwer Health)
2 publications, 1.65%
|
|
|
American Physiological Society
2 publications, 1.65%
|
|
|
Georg Thieme Verlag KG
2 publications, 1.65%
|
|
|
CSIRO Publishing
1 publication, 0.83%
|
|
|
Society for the Study of Reproduction
1 publication, 0.83%
|
|
|
Proceedings of the National Academy of Sciences (PNAS)
1 publication, 0.83%
|
|
|
American Society of Hematology
1 publication, 0.83%
|
|
|
Rockefeller University Press
1 publication, 0.83%
|
|
|
American Association for the Advancement of Science (AAAS)
1 publication, 0.83%
|
|
|
Future Medicine
1 publication, 0.83%
|
|
|
Autonomous Non-profit Organization Editorial Board of the journal Uspekhi Khimii
1 publication, 0.83%
|
|
|
5
10
15
20
25
|
- We do not take into account publications without a DOI.
- Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
- Statistics recalculated weekly.
Are you a researcher?
Create a profile to get free access to personal recommendations for colleagues and new articles.
Metrics
Cite this
GOST |
RIS |
BibTex |
MLA
Cite this
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)
Copy
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
Copy
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 - Proffitt, Chris
AU - Bliesath, Josh
AU - Siddiqui-Jain, Adam
AU - Omori, May
AU - Huser, Nanni
AU - Rice, William G
AU - Ryckman, David M.
AU - Anderes, Kenna
PY - 2012
DA - 2012/06/08
PB - American Chemical Society (ACS)
SP - 602-606
IS - 7
VL - 3
PMID - 24900516
SN - 1948-5875
SN - 1948-5875
ER -
Cite this
BibTex
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 Chris Proffitt and Josh Bliesath and Adam Siddiqui-Jain and May Omori and Nanni Huser and William G Rice and David M. Ryckman and Kenna Anderes},
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.