New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (N

Zahid, Huda; Buchholz, Caroline R.; Singh, Manjulata; Ciccone, Michael F.; Chan, Alice; Nithianantham, Stanley; Shi, Ke; Aihara, Hideki; Fischer, Marcus; Schonbrunn, Ernst; dos Santos, Camila O.; Landry, Joseph W.; Pomerantz, William C.K.

doi:10.1021/acs.jmedchem.1c01294

New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (N

Journal Article · 01 September 2021 · J. Med. Chem.

DOI:https://doi.org/10.1021/acs.jmedchem.1c01294· OSTI ID:1828955

Zahid, Huda; Buchholz, Caroline R.; Singh, Manjulata; Ciccone, Michael F.; Chan, Alice; Nithianantham, Stanley; Shi, Ke; Aihara, Hideki; Fischer, Marcus; Schonbrunn, Ernst; dos Santos, Camila O.; Landry, Joseph W.; Pomerantz, William C.K.

Research Organization:: Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)

Sponsoring Organization:: DOE - Office Of Science; National Institutes of Health (NIH)

OSTI ID:: 1828955

Journal Information:: J. Med. Chem., Vol. 64, Issue (18)

Country of Publication:: United States

Language:: ENGLISH

References (48)

Epigenetics: A Landscape Takes Shape No authors listed Cell https://doi.org/10.1016/j.cell.2007.02.006		February 2007
The molecular hallmarks of epigenetic control No authors listed Nature Reviews Genetics https://doi.org/10.1038/nrg.2016.59		June 2016
Mechanisms of action and regulation of ATP-dependent chromatin-remodelling complexes No authors listed Nature Reviews Molecular Cell Biology https://doi.org/10.1038/nrm.2017.26		May 2017
A rationale to target the SWI/SNF complex for cancer therapy No authors listed Trends in Genetics https://doi.org/10.1016/j.tig.2014.05.001		August 2014
Mammalian SWI/SNF complexes in cancer: emerging therapeutic opportunities No authors listed Current Opinion in Genetics & Development https://doi.org/10.1016/j.gde.2017.02.004		February 2017
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7 No authors listed Journal of Medicinal Chemistry https://doi.org/10.1021/acs.jmedchem.8b01413		December 2018
Isolation of human NURF: a regulator of Engrailed gene expression No authors listed The EMBO Journal https://doi.org/10.1093/emboj/cdg582		November 2003
Opportunity knocks for uncovering the new function of an understudied nucleosome remodeling complex member, the bromodomain PHD finger transcription factor, BPTF No authors listed Current Opinion in Chemical Biology https://doi.org/10.1016/j.cbpa.2021.02.003		August 2021
Dual Functions of Largest NURF Subunit NURF301 in Nucleosome Sliding and Transcription Factor Interactions No authors listed Molecular Cell https://doi.org/10.1016/S1097-2765(01)00345-8		September 2001
Identification and Characterization of BPTF, a Novel Bromodomain Transcription Factor No authors listed Genomics https://doi.org/10.1006/geno.1999.6070		January 2000
Recognition of a Mononucleosomal Histone Modification Pattern by BPTF via Multivalent Interactions No authors listed Cell https://doi.org/10.1016/j.cell.2011.03.053		May 2011
Essential Role of Chromatin Remodeling Protein Bptf in Early Mouse Embryos and Embryonic Stem Cells No authors listed PLoS Genetics https://doi.org/10.1371/journal.pgen.1000241		October 2008
BPTF Is Essential for T Cell Homeostasis and Function No authors listed The Journal of Immunology https://doi.org/10.4049/jimmunol.1600642		October 2016
BPTF Maintains Chromatin Accessibility and the Self-Renewal Capacity of Mammary Gland Stem Cells No authors listed Stem Cell Reports https://doi.org/10.1016/j.stemcr.2017.04.031		July 2017
The Role of BPTF in Melanoma Progression and in Response to BRAF-Targeted Therapy No authors listed JNCI: Journal of the National Cancer Institute https://doi.org/10.1093/jnci/djv034		February 2015
Chromatin-Remodelling Complex NURF Is Essential for Differentiation of Adult Melanocyte Stem Cells No authors listed PLOS Genetics https://doi.org/10.1371/journal.pgen.1005555		October 2015
BPTF is required for c-MYC transcriptional activity and in vivo tumorigenesis No authors listed Nature Communications https://doi.org/10.1038/ncomms10153		January 2016
c-MYC partners with BPTF in human cancer No authors listed Molecular & Cellular Oncology https://doi.org/10.1080/23723556.2016.1152346		May 2016
BPTF promotes tumor growth and predicts poor prognosis in lung adenocarcinomas No authors listed Oncotarget https://doi.org/10.18632/oncotarget.5302		September 2015
BPTF, a chromatin remodeling-related gene, exhibits frameshift mutations in gastric and colorectal cancers No authors listed APMIS https://doi.org/10.1111/apm.12512		February 2016
BPTF regulates growth of adult and pediatric high-grade glioma through the MYC pathway No authors listed Oncogene https://doi.org/10.1038/s41388-019-1125-7		December 2019
Bromodomain PHD‑finger transcription factor promotes glioma progression and indicates poor prognosis No authors listed Oncology Reports https://doi.org/10.3892/or.2018.6832		October 2018
BPTF promotes hepatocellular carcinoma growth by modulating hTERT signaling and cancer stem cell traits No authors listed Redox Biology https://doi.org/10.1016/j.redox.2018.10.018		January 2019
Druggability Analysis and Structural Classification of Bromodomain Acetyl-lysine Binding Sites No authors listed Journal of Medicinal Chemistry https://doi.org/10.1021/jm300346w		July 2012
Domain-selective targeting of BET proteins in cancer and immunological diseases No authors listed Current Opinion in Chemical Biology https://doi.org/10.1016/j.cbpa.2020.02.003		August 2020
Advancements in the Development of non‐BET Bromodomain Chemical Probes No authors listed ChemMedChem https://doi.org/10.1002/cmdc.201800738		January 2019
Dual Screening of BPTF and Brd4 Using Protein-Observed Fluorine NMR Uncovers New Bromodomain Probe Molecules No authors listed ACS Chemical Biology https://doi.org/10.1021/acschembio.5b00483		July 2015
BET domain co-regulators in obesity, inflammation and cancer No authors listed Nature Reviews Cancer https://doi.org/10.1038/nrc3256		June 2012
Selectivity, ligand deconstruction, and cellular activity analysis of a BPTF bromodomain inhibitor No authors listed Organic & Biomolecular Chemistry https://doi.org/10.1039/C8OB02599A		January 2019
Autophagy-Dependent Sensitization of Triple-Negative Breast Cancer Models to Topoisomerase II Poisons by Inhibition of the Nucleosome Remodeling Factor No authors listed Molecular Cancer Research https://doi.org/10.1158/1541-7786.MCR-20-0743		April 2021
Synthesis of NVS-BPTF-1 and evaluation of its biological activity No authors listed Bioorganic & Medicinal Chemistry Letters https://doi.org/10.1016/j.bmcl.2021.128208		September 2021
Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe No authors listed Journal of Medicinal Chemistry https://doi.org/10.1021/acs.jmedchem.6b01566		January 2017
New inhibitors for the BPTF bromodomain enabled by structural biology and biophysical assay development No authors listed Organic & Biomolecular Chemistry https://doi.org/10.1039/D0OB00506A		January 2020
Fluorinated Aromatic Amino Acids Are Sensitive ¹⁹ F NMR Probes for Bromodomain-Ligand Interactions No authors listed ACS Chemical Biology https://doi.org/10.1021/cb5007344		October 2014
The role of ligand efficiency metrics in drug discovery No authors listed Nature Reviews Drug Discovery https://doi.org/10.1038/nrd4163		January 2014
Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains No authors listed Journal of Medicinal Chemistry https://doi.org/10.1021/acs.jmedchem.0c00075		May 2020
Cell permeability beyond the rule of 5 No authors listed Advanced Drug Delivery Reviews https://doi.org/10.1016/j.addr.2016.03.013		June 2016
Selective N‐Terminal BET Bromodomain Inhibitors by Targeting Non‐Conserved Residues and Structured Water Displacement** No authors listed Angewandte Chemie International Edition https://doi.org/10.1002/anie.202008625		November 2020
Discovery of selective BPTF bromodomain inhibitors by screening and structure-based optimization No authors listed Biochemical and Biophysical Research Communications https://doi.org/10.1016/j.bbrc.2021.01.067		March 2021
BPTF Depletion Enhances T-cell–Mediated Antitumor Immunity No authors listed Cancer Research https://doi.org/10.1158/0008-5472.CAN-15-3125		September 2016
Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials No authors listed Science Translational Medicine https://doi.org/10.1126/scitranslmed.aaw8412		September 2019
Sustained activation of STAT5 is essential for chromatin remodeling and maintenance of mammary-specific function No authors listed The Journal of Cell Biology https://doi.org/10.1083/jcb.200807021		January 2009
Differentiation of Mouse Breast Epithelial HC11 and EpH4 Cells No authors listed Journal of Visualized Experiments https://doi.org/10.3791/60147		January 2020
Systematically Mitigating the p38α Activity of Triazole-based BET Inhibitors No authors listed ACS Medicinal Chemistry Letters https://doi.org/10.1021/acsmedchemlett.9b00227		August 2019
XDS No authors listed Acta Crystallographica Section D Biological Crystallography https://doi.org/10.1107/S0907444909047337		January 2010
PHENIX: a comprehensive Python-based system for macromolecular structure solution No authors listed Acta Crystallographica Section D Biological Crystallography https://doi.org/10.1107/S0907444909052925		January 2010
Features and development of Coot No authors listed Acta Crystallographica Section D Biological Crystallography https://doi.org/10.1107/S0907444910007493		March 2010
Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family No authors listed Cell https://doi.org/10.1016/j.cell.2012.02.013		March 2012

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