Fragment-based screening of the bromodomain of ATAD2

Harner, Mary J.; Chauder, Brian A.; Phan, Jason; Fesik, Stephen W.

doi:10.1021/jm501035j

Title: Fragment-based screening of the bromodomain of ATAD2

Abstract

Cellular and genetic evidence suggest that inhibition of ATAD2 could be a useful strategy to treat several types of cancer. To discover small-molecule inhibitors of the bromodomain of ATAD2, we used a fragment-based approach. As a result, fragment hits were identified using NMR spectroscopy, and ATAD2 was crystallized with three of the hits identified in the fragment screen.

Authors:

Harner, Mary J. ^[1]; Chauder, Brian A. ^[1]; Phan, Jason ^[1]; Fesik, Stephen W. ^[1]

Vanderbilt Univ. School of Medicine, Nashville, TN (United States)

Publication Date:: Tue Oct 14 00:00:00 EDT 2014

Research Org.:: Vanderbilt Univ. School of Medicine, Nashville, TN (United States)

Sponsoring Org.:: USDOE Office of Science (SC)

OSTI Identifier:: 1346018

Grant/Contract Number:: AC02-06CH11357

Resource Type:: Accepted Manuscript

Journal Name:: Journal of Medicinal Chemistry

Additional Journal Information:: Journal Volume: 57; Journal Issue: 22; Journal ID: ISSN 0022-2623

Publisher:: American Chemical Society (ACS)

Country of Publication:: United States

Language:: English

Subject:: 59 BASIC BIOLOGICAL SCIENCES; 60 APPLIED LIFE SCIENCES

Citation Formats


                    Harner, Mary J., Chauder, Brian A., Phan, Jason, and Fesik, Stephen W. Fragment-based screening of the bromodomain of ATAD2.  United States: N. p., 2014. 
Web.  doi:10.1021/jm501035j.

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                    Harner, Mary J., Chauder, Brian A., Phan, Jason, & Fesik, Stephen W. Fragment-based screening of the bromodomain of ATAD2.  United States.  https://doi.org/10.1021/jm501035j

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                    Harner, Mary J., Chauder, Brian A., Phan, Jason, and Fesik, Stephen W. Tue .  
"Fragment-based screening of the bromodomain of ATAD2".  United States.  https://doi.org/10.1021/jm501035j.  https://www.osti.gov/servlets/purl/1346018.

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@article{osti_1346018,

  title        = {Fragment-based screening of the bromodomain of ATAD2},

  author       = {Harner, Mary J. and Chauder, Brian A. and Phan, Jason and Fesik, Stephen W.},

  abstractNote = {Cellular and genetic evidence suggest that inhibition of ATAD2 could be a useful strategy to treat several types of cancer. To discover small-molecule inhibitors of the bromodomain of ATAD2, we used a fragment-based approach. As a result, fragment hits were identified using NMR spectroscopy, and ATAD2 was crystallized with three of the hits identified in the fragment screen.},

  doi          = {10.1021/jm501035j},

  journal      = {Journal of Medicinal Chemistry},

  number       = 22,

  volume       = 57,

  place        = {United States},

  year         = {Tue Oct 14 00:00:00 EDT 2014},

  month        = {Tue Oct 14 00:00:00 EDT 2014}

}

Copy to clipboard

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https://doi.org/10.1021/jm501035j

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Works referenced in this record:

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Filippakopoulos, Panagis; Knapp, Stefan
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Druggability Indices for Protein Targets Derived from NMR-Based Screening Data
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Hajduk, Philip J.; Huth, Jeffrey R.; Fesik, Stephen W.
Journal of Medicinal Chemistry, Vol. 48, Issue 7
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Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain
journal, December 2013

Ferguson, Fleur M.; Fedorov, Oleg; Chaikuad, Apirat
Journal of Medicinal Chemistry, Vol. 56, Issue 24
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Targeting bromodomains: epigenetic readers of lysine acetylation
journal, April 2014

Filippakopoulos, Panagis; Knapp, Stefan
Nature Reviews Drug Discovery, Vol. 13, Issue 5
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Functional characterization of ATAD2 as a new cancer/testis factor and a predictor of poor prognosis in breast and lung cancers
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Caron, C.; Lestrat, C.; Marsal, S.
Oncogene, Vol. 29, Issue 37
DOI: 10.1038/onc.2010.259

ANCCA, an estrogen-regulated AAA+ ATPase coactivator for ER , is required for coregulator occupancy and chromatin modification
journal, November 2007

Zou, J. X.; Revenko, A. S.; Li, L. B.
Proceedings of the National Academy of Sciences, Vol. 104, Issue 46
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Shuker, S. B.; Hajduk, P. J.; Meadows, R. P.
Science, Vol. 274, Issue 5292, p. 1531-1534
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Chromatin Loading of E2F-MLL Complex by Cancer-Associated Coregulator ANCCA via Reading a Specific Histone Mark
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Deregulated E2F and the AAA+ Coregulator ANCCA Drive Proto-Oncogene ACTR/AIB1 Overexpression in Breast Cancer
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Works referencing / citing this record:

Disulfide bridge formation influences ligand recognition by the ATAD2 bromodomain
journal, December 2018

Gay, Jamie C.; Eckenroth, Brian E.; Evans, Chiara M.
Proteins: Structure, Function, and Bioinformatics, Vol. 87, Issue 2
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Hussain, Muzammal; Zhou, Yang; Song, Yu
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Chemische Epigenetik: der Einfluss chemischer und chemo‐biologischer Techniken auf die Zielstruktur‐Validierung von Bromodomänen
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Schiedel, Matthias; Moroglu, Mustafa; Ascough, David M. H.
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Overexpression of microRNA‐186 inhibits angiogenesis in retinoblastoma via the Hedgehog signaling pathway by targeting ATAD2
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Wu, Shuai; Han, Mei; Zhang, Chao
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Chemical Epigenetics: The Impact of Chemical and Chemical Biology Techniques on Bromodomain Target Validation
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Schiedel, Matthias; Moroglu, Mustafa; Ascough, David M. H.
Angewandte Chemie International Edition, Vol. 58, Issue 50
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Cochran, Andrea G.; Conery, Andrew R.; Sims, Robert J.
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Organic & Biomolecular Chemistry, Vol. 16, Issue 11
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Bromodomain biology and drug discovery
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The identification of new ATAD2 bromodomain inhibitors: the application of combined ligand and structure-based virtual screening
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Synthesis and Demonstration of the Biological Relevance of sp ³ -rich Scaffolds Distantly Related to Natural Product Frameworks
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Insights Into the Allosteric Inhibition of the SUMO E2 Enzyme Ubc9
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Hewitt, William M.; Lountos, George T.; Zlotkowski, Katherine
Angewandte Chemie, Vol. 128, Issue 19
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Disulfide bridge formation influences ligand recognition by the ATAD2 bromodomain
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Gay, Jamie C.; Eckenroth, Brian E.; Evans, Chiara M.
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Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition
journal, April 2015

Theodoulou, Natalie H.; Bamborough, Paul; Bannister, Andrew J.
Journal of Medicinal Chemistry, Vol. 59, Issue 4
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Similar Records

Title: Fragment-based screening of the bromodomain of ATAD2

Abstract

Citation Formats

Targeting bromodomains: epigenetic readers of lysine acetylation journal, April 2014

Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain journal, December 2013

Functional characterization of ATAD2 as a new cancer/testis factor and a predictor of poor prognosis in breast and lung cancers journal, June 2010

Significance of PRO2000/ANCCA expression, a novel proliferation-associated protein in hepatocellular carcinoma journal, January 2014

ANCCA, an estrogen-regulated AAA+ ATPase coactivator for ER , is required for coregulator occupancy and chromatin modification journal, November 2007

Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites journal, July 2012

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family journal, March 2012

DRUG DESIGN: Discovering High-Affinity Ligands for Proteins journal, October 1997

Discovering High-Affinity Ligands for Proteins: SAR by NMR journal, November 1996

Fragment-based drug discovery using NMR spectroscopy journal, May 2013

Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain journal, January 2014

Druggability Indices for Protein Targets Derived from NMR-Based Screening Data journal, April 2005

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors journal, March 2014

Fragment-based drug discovery using NMR spectroscopy journal, May 2013

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family journal, March 2012

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors journal, March 2014

Druggability Indices for Protein Targets Derived from NMR-Based Screening Data journal, April 2005

Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain journal, December 2013

Targeting bromodomains: epigenetic readers of lysine acetylation journal, April 2014

Functional characterization of ATAD2 as a new cancer/testis factor and a predictor of poor prognosis in breast and lung cancers journal, June 2010

ANCCA, an estrogen-regulated AAA+ ATPase coactivator for ER , is required for coregulator occupancy and chromatin modification journal, November 2007

Discovering High-Affinity Ligands for Proteins: SAR by NMR journal, November 1996

Chromatin Loading of E2F-MLL Complex by Cancer-Associated Coregulator ANCCA via Reading a Specific Histone Mark journal, November 2010

Androgen-Induced Coactivator ANCCA Mediates Specific Androgen Receptor Signaling in Prostate Cancer journal, March 2009

ATAD2 Is a Novel Cofactor for MYC, Overexpressed and Amplified in Aggressive Tumors journal, October 2009

ANCCA/ATAD2 Overexpression Identifies Breast Cancer Patients with Poor Prognosis, Acting to Drive Proliferation and Survival of Triple-Negative Cells through Control of B-Myb and EZH2 journal, September 2010

Deregulated E2F and the AAA+ Coregulator ANCCA Drive Proto-Oncogene ACTR/AIB1 Overexpression in Breast Cancer journal, February 2010

Disulfide bridge formation influences ligand recognition by the ATAD2 bromodomain journal, December 2018

ATAD2 in cancer: a pharmacologically challenging but tractable target journal, November 2017

Insights Into the Allosteric Inhibition of the SUMO E2 Enzyme Ubc9 journal, April 2016

Chemische Epigenetik: der Einfluss chemischer und chemo‐biologischer Techniken auf die Zielstruktur‐Validierung von Bromodomänen journal, November 2019

Overexpression of microRNA‐186 inhibits angiogenesis in retinoblastoma via the Hedgehog signaling pathway by targeting ATAD2 journal, February 2019

Chemical Epigenetics: The Impact of Chemical and Chemical Biology Techniques on Bromodomain Target Validation journal, December 2019

Bromodomains: a new target class for drug development journal, July 2019

Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach journal, January 2018

Bromodomain biology and drug discovery journal, October 2019

The identification of new ATAD2 bromodomain inhibitors: the application of combined ligand and structure-based virtual screening journal, December 2017

ATAD2 overexpression is associated with progression and prognosis in colorectal cancer journal, January 2016

Observed bromodomain flexibility reveals histone peptide- and small molecule ligand-compatible forms of ATAD2 journal, February 2015

Synthesis and Demonstration of the Biological Relevance of sp 3 -rich Scaffolds Distantly Related to Natural Product Frameworks journal, October 2017

Insights Into the Allosteric Inhibition of the SUMO E2 Enzyme Ubc9 journal, April 2016

Disulfide bridge formation influences ligand recognition by the ATAD2 bromodomain text, January 2019

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition journal, April 2015

Targeting bromodomains: epigenetic readers of lysine acetylation
journal, April 2014

Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain
journal, December 2013

Functional characterization of ATAD2 as a new cancer/testis factor and a predictor of poor prognosis in breast and lung cancers
journal, June 2010

Significance of PRO2000/ANCCA expression, a novel proliferation-associated protein in hepatocellular carcinoma
journal, January 2014

ANCCA, an estrogen-regulated AAA+ ATPase coactivator for ER , is required for coregulator occupancy and chromatin modification
journal, November 2007

Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites
journal, July 2012

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family
journal, March 2012

DRUG DESIGN: Discovering High-Affinity Ligands for Proteins
journal, October 1997

Discovering High-Affinity Ligands for Proteins: SAR by NMR
journal, November 1996

Fragment-based drug discovery using NMR spectroscopy
journal, May 2013

Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain
journal, January 2014

Druggability Indices for Protein Targets Derived from NMR-Based Screening Data
journal, April 2005

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors
journal, March 2014

Fragment-based drug discovery using NMR spectroscopy
journal, May 2013

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family
journal, March 2012

Acetyl-lysine Binding Site of Bromodomain-Containing Protein 4 (BRD4) Interacts with Diverse Kinase Inhibitors
journal, March 2014

Druggability Indices for Protein Targets Derived from NMR-Based Screening Data
journal, April 2005

Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain
journal, December 2013

Targeting bromodomains: epigenetic readers of lysine acetylation
journal, April 2014

Functional characterization of ATAD2 as a new cancer/testis factor and a predictor of poor prognosis in breast and lung cancers
journal, June 2010

ANCCA, an estrogen-regulated AAA+ ATPase coactivator for ER , is required for coregulator occupancy and chromatin modification
journal, November 2007

Discovering High-Affinity Ligands for Proteins: SAR by NMR
journal, November 1996

Chromatin Loading of E2F-MLL Complex by Cancer-Associated Coregulator ANCCA via Reading a Specific Histone Mark
journal, November 2010

Androgen-Induced Coactivator ANCCA Mediates Specific Androgen Receptor Signaling in Prostate Cancer
journal, March 2009

ATAD2 Is a Novel Cofactor for MYC, Overexpressed and Amplified in Aggressive Tumors
journal, October 2009

ANCCA/ATAD2 Overexpression Identifies Breast Cancer Patients with Poor Prognosis, Acting to Drive Proliferation and Survival of Triple-Negative Cells through Control of B-Myb and EZH2
journal, September 2010

Deregulated E2F and the AAA+ Coregulator ANCCA Drive Proto-Oncogene ACTR/AIB1 Overexpression in Breast Cancer
journal, February 2010

Disulfide bridge formation influences ligand recognition by the ATAD2 bromodomain
journal, December 2018

ATAD2 in cancer: a pharmacologically challenging but tractable target
journal, November 2017

Insights Into the Allosteric Inhibition of the SUMO E2 Enzyme Ubc9
journal, April 2016

Chemische Epigenetik: der Einfluss chemischer und chemo‐biologischer Techniken auf die Zielstruktur‐Validierung von Bromodomänen
journal, November 2019

Overexpression of microRNA‐186 inhibits angiogenesis in retinoblastoma via the Hedgehog signaling pathway by targeting ATAD2
journal, February 2019

Chemical Epigenetics: The Impact of Chemical and Chemical Biology Techniques on Bromodomain Target Validation
journal, December 2019

Bromodomains: a new target class for drug development
journal, July 2019

Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach
journal, January 2018

Bromodomain biology and drug discovery
journal, October 2019

The identification of new ATAD2 bromodomain inhibitors: the application of combined ligand and structure-based virtual screening
journal, December 2017

ATAD2 overexpression is associated with progression and prognosis in colorectal cancer
journal, January 2016

Observed bromodomain flexibility reveals histone peptide- and small molecule ligand-compatible forms of ATAD2
journal, February 2015

Synthesis and Demonstration of the Biological Relevance of sp ³ -rich Scaffolds Distantly Related to Natural Product Frameworks
journal, October 2017

Insights Into the Allosteric Inhibition of the SUMO E2 Enzyme Ubc9
journal, April 2016

Disulfide bridge formation influences ligand recognition by the ATAD2 bromodomain
text, January 2019

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition
journal, April 2015