From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors
- Authors:
- more »
- Publication Date:
- Sponsoring Org.:
- USDOE
- OSTI Identifier:
- 1413842
- Grant/Contract Number:
- AC02-06CH11357; AC02-05CH11231
- Resource Type:
- Publisher's Accepted Manuscript
- Journal Name:
- Bioorganic and Medicinal Chemistry Letters
- Additional Journal Information:
- Journal Name: Bioorganic and Medicinal Chemistry Letters Journal Volume: 27 Journal Issue: 13; Journal ID: ISSN 0960-894X
- Publisher:
- Elsevier
- Country of Publication:
- United Kingdom
- Language:
- English
Citation Formats
Liang, Jun, Labadie, Sharada, Zhang, Birong, Ortwine, Daniel F., Patel, Snahel, Vinogradova, Maia, Kiefer, James R., Mauer, Till, Gehling, Victor S., Harmange, Jean-Christophe, Cummings, Richard, Lai, Tommy, Liao, Jiangpeng, Zheng, Xiaoping, Liu, Yichin, Gustafson, Amy, Van der Porten, Erica, Mao, Weifeng, Liederer, Bianca M., Deshmukh, Gauri, An, Le, Ran, Yingqing, Classon, Marie, Trojer, Patrick, Dragovich, Peter S., and Murray, Lesley. From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors. United Kingdom: N. p., 2017.
Web. doi:10.1016/j.bmcl.2017.05.016.
Liang, Jun, Labadie, Sharada, Zhang, Birong, Ortwine, Daniel F., Patel, Snahel, Vinogradova, Maia, Kiefer, James R., Mauer, Till, Gehling, Victor S., Harmange, Jean-Christophe, Cummings, Richard, Lai, Tommy, Liao, Jiangpeng, Zheng, Xiaoping, Liu, Yichin, Gustafson, Amy, Van der Porten, Erica, Mao, Weifeng, Liederer, Bianca M., Deshmukh, Gauri, An, Le, Ran, Yingqing, Classon, Marie, Trojer, Patrick, Dragovich, Peter S., & Murray, Lesley. From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors. United Kingdom. https://doi.org/10.1016/j.bmcl.2017.05.016
Liang, Jun, Labadie, Sharada, Zhang, Birong, Ortwine, Daniel F., Patel, Snahel, Vinogradova, Maia, Kiefer, James R., Mauer, Till, Gehling, Victor S., Harmange, Jean-Christophe, Cummings, Richard, Lai, Tommy, Liao, Jiangpeng, Zheng, Xiaoping, Liu, Yichin, Gustafson, Amy, Van der Porten, Erica, Mao, Weifeng, Liederer, Bianca M., Deshmukh, Gauri, An, Le, Ran, Yingqing, Classon, Marie, Trojer, Patrick, Dragovich, Peter S., and Murray, Lesley. Sat .
"From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors". United Kingdom. https://doi.org/10.1016/j.bmcl.2017.05.016.
@article{osti_1413842,
title = {From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors},
author = {Liang, Jun and Labadie, Sharada and Zhang, Birong and Ortwine, Daniel F. and Patel, Snahel and Vinogradova, Maia and Kiefer, James R. and Mauer, Till and Gehling, Victor S. and Harmange, Jean-Christophe and Cummings, Richard and Lai, Tommy and Liao, Jiangpeng and Zheng, Xiaoping and Liu, Yichin and Gustafson, Amy and Van der Porten, Erica and Mao, Weifeng and Liederer, Bianca M. and Deshmukh, Gauri and An, Le and Ran, Yingqing and Classon, Marie and Trojer, Patrick and Dragovich, Peter S. and Murray, Lesley},
abstractNote = {},
doi = {10.1016/j.bmcl.2017.05.016},
journal = {Bioorganic and Medicinal Chemistry Letters},
number = 13,
volume = 27,
place = {United Kingdom},
year = {Sat Jul 01 00:00:00 EDT 2017},
month = {Sat Jul 01 00:00:00 EDT 2017}
}
Free Publicly Available Full Text
Publisher's Version of Record
https://doi.org/10.1016/j.bmcl.2017.05.016
https://doi.org/10.1016/j.bmcl.2017.05.016
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Cited by: 36 works
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Works referenced in this record:
8-Substituted Pyrido[3,4- d ]pyrimidin-4(3 H )-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors
journal, April 2015
- Bavetsias, Vassilios; Lanigan, Rachel M.; Ruda, Gian Filippo
- Journal of Medicinal Chemistry, Vol. 59, Issue 4
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives
journal, April 2015
- Westaway, Susan M.; Preston, Alex G. S.; Barker, Michael D.
- Journal of Medicinal Chemistry, Vol. 59, Issue 4
Structural analysis of human KDM5B guides histone demethylase inhibitor development
journal, May 2016
- Johansson, Catrine; Velupillai, Srikannathasan; Tumber, Anthony
- Nature Chemical Biology, Vol. 12, Issue 7
Ligand efficiency: a useful metric for lead selection
journal, May 2004
- Hopkins, Andrew L.; Groom, Colin R.; Alex, Alexander
- Drug Discovery Today, Vol. 9, Issue 10
Recent Progress in Histone Demethylase Inhibitors
journal, April 2015
- McAllister, Tom E.; England, Katherine S.; Hopkinson, Richard J.
- Journal of Medicinal Chemistry, Vol. 59, Issue 4
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4- d ]pyrimidin-4(3 H )-one Derivatives
journal, April 2015
- Westaway, Susan M.; Preston, Alex G. S.; Barker, Michael D.
- Journal of Medicinal Chemistry, Vol. 59, Issue 4
An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells
journal, May 2016
- Vinogradova, Maia; Gehling, Victor S.; Gustafson, Amy
- Nature Chemical Biology, Vol. 12, Issue 7
The influence of drug-like concepts on decision-making in medicinal chemistry
journal, November 2007
- Leeson, Paul D.; Springthorpe, Brian
- Nature Reviews Drug Discovery, Vol. 6, Issue 11
Overcoming Intrinsic Multidrug Resistance in Melanoma by Blocking the Mitochondrial Respiratory Chain of Slow-Cycling JARID1Bhigh Cells
journal, June 2013
- Roesch, Alexander; Vultur, Adina; Bogeski, Ivan
- Cancer Cell, Vol. 23, Issue 6
The putative oncogene GASC1 demethylates tri- and dimethylated lysine 9 on histone H3
journal, May 2006
- Cloos, Paul A. C.; Christensen, Jesper; Agger, Karl
- Nature, Vol. 442, Issue 7100
Structural basis for histone H3 Lys 27 demethylation by UTX/KDM6A
journal, October 2011
- Sengoku, T.; Yokoyama, S.
- Genes & Development, Vol. 25, Issue 21
Rapid NMR-based functional screening and IC50 measurements performed at unprecedentedly low enzyme concentration
journal, January 2005
- Dalvit, Claudio; Papeo, Gianluca; Mongelli, Nicola
- Drug Development Research, Vol. 64, Issue 2
Histone lysine demethylases as targets for anticancer therapy
journal, November 2013
- Højfeldt, Jonas W.; Agger, Karl; Helin, Kristian
- Nature Reviews Drug Discovery, Vol. 12, Issue 12
Identification of potent, selective KDM5 inhibitors
journal, September 2016
- Gehling, Victor S.; Bellon, Steven F.; Harmange, Jean-Christophe
- Bioorganic & Medicinal Chemistry Letters, Vol. 26, Issue 17
Molecular mechanisms and potential functions of histone demethylases
journal, April 2012
- Kooistra, Susanne Marije; Helin, Kristian
- Nature Reviews Molecular Cell Biology, Vol. 13, Issue 5
Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies
journal, August 2016
- Liang, Jun; Zhang, Birong; Labadie, Sharada
- Bioorganic & Medicinal Chemistry Letters, Vol. 26, Issue 16
Histone methylation: a dynamic mark in health, disease and inheritance
journal, April 2012
- Greer, Eric L.; Shi, Yang
- Nature Reviews Genetics, Vol. 13, Issue 5
Inhibitors of histone demethylases
journal, June 2011
- Lohse, Brian; Kristensen, Jesper L.; Kristensen, Line H.
- Bioorganic & Medicinal Chemistry, Vol. 19, Issue 12
Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors
journal, September 2016
- Labadie, Sharada S.; Dragovich, Peter S.; Cummings, Richard T.
- Bioorganic & Medicinal Chemistry Letters, Vol. 26, Issue 18
Lysine Demethylases Inhibitors
journal, December 2011
- Suzuki, Takayoshi; Miyata, Naoki
- Journal of Medicinal Chemistry, Vol. 54, Issue 24
Inhibitors of histone deacetylase as antitumor agents: A critical review
journal, August 2016
- Manal, Mohammed; Chandrasekar, M. J. N.; Gomathi Priya, Jeyapal
- Bioorganic Chemistry, Vol. 67
Histone Lysine Methylation Dynamics: Establishment, Regulation, and Biological Impact
journal, November 2012
- Black, Joshua C.; Van Rechem, Capucine; Whetstine, Johnathan R.
- Molecular Cell, Vol. 48, Issue 4
Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds
journal, July 2016
- Horton, John R.; Liu, Xu; Gale, Molly
- Cell Chemical Biology, Vol. 23, Issue 7
Histone deacetylases and cancer: causes and therapies
journal, December 2001
- Marks, Paul A.; Rifkind, Richard A.; Richon, Victoria M.
- Nature Reviews Cancer, Vol. 1, Issue 3
Chromatin structure and the inheritance of epigenetic information
journal, April 2010
- Margueron, Raphaël; Reinberg, Danny
- Nature Reviews Genetics, Vol. 11, Issue 4
Small-molecular modulators of cancer-associated epigenetic mechanisms
journal, January 2013
- Itoh, Yukihiro; Suzuki, Takayoshi; Miyata, Naoki
- Molecular BioSystems, Vol. 9, Issue 5
A Chromatin-Mediated Reversible Drug-Tolerant State in Cancer Cell Subpopulations
journal, April 2010
- Sharma, Sreenath V.; Lee, Diana Y.; Li, Bihua
- Cell, Vol. 141, Issue 1