ArticleACS chemical biology2020
Optimization of Ligands Using Focused DNA-Encoded Libraries To Develop a Selective, Cell-Permeable CBX8 Chromodomain Inhibitor.
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Article in ACS chemical biology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers.
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Who cites it
42 citing papers in PubMed, 84 citations in OpenAlex.
- Unleashing the power of DNA-encoded libraries for challenging targets in drug discovery.Pharmaceutical science advances · 2026Review
- Inhibition of USP7 Destabilizes the Noncanonical PRC1.1 Complex and Induces Neuroblastoma Differentiation.Molecular cancer research : MCR · 2026Article
- Covalent Protein Inhibitors via Tyrosine and Tryptophan Conjugation with Cyclic Imine Mannich Electrophiles.Angewandte Chemie (International ed. in English) · 2026Article
- Structural landscape of H3K27me3 recognition by protein domains and their potential for inhibition.The Journal of biological chemistry · 2026Review
- CBX8 suppresses autophagy-dependent senescence in colorectal cancer by modulating the mTOR signaling pathway.International journal of biological sciences · 2026Article
- Epigenetic reader chromodomain as a potential therapeutic target.RSC chemical biology · 2025Review
- Regulatory roles of non-coding RNAs in programmed cell death pathways and drug resistance in gastrointestinal stromal tumors.Clinical and experimental medicine · 2025Review
- Unravelling the impact of the chromobox proteins in human cancers.Cell death & disease · 2025Review
- Epigenetic regulatory protein chromobox family regulates multiple signalling pathways and mechanisms in cancer.Clinical epigenetics · 2025Review
- Evaluating the Diversity and Target Addressability of DELs using Scaffold Analysis and Machine Learning.ACS medicinal chemistry letters · 2025Article
- Pharmacological targeting of CBX7 alters the epigenetic landscape and induces differentiation of leukemic cells.Blood neoplasia · 2024Article
- How CBX proteins regulate normal and leukemic blood cells.FEBS letters · 2024Review
- A Fragment-Based Screen for Inhibitors of Escherichia coli N5-CAIR Mutase.Research square · 2024Article
- Pharmacological targeting of the cancer epigenome.Nature cancer · 2024Review
- Investigating the Cytosolic Delivery of Proteins by Lipid Nanoparticles Using the Chloroalkane Penetration Assay.Biochemistry · 2024Article
- Exploiting the Carboxylate-Binding Pocket of β-Lactamase Enzymes Using a Focused DNA-Encoded Chemical Library.Journal of medicinal chemistry · 2024Article
- CBX8 Promotes Epithelial-mesenchymal Transition, Migration, and Invasion of Lung Cancer through Wnt/β-catenin Signaling Pathway.Current protein & peptide science · 2024Article
- Small-molecule discovery through DNA-encoded libraries.Nature reviews. Drug discovery · 2023Review
- Chemical tools targeting readers of lysine methylation.Current opinion in chemical biology · 2023Review
- Combining pharmacophore models derived from DNA-encoded chemical libraries with structure-based exploration to predict Tankyrase 1 inhibitors.European journal of medicinal chemistry · 2023Article
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 2 countries.
Sijie WangDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy , Purdue University and Purdue University Center for Cancer Research , 575 Stadium Mall Drive , West Lafayette , Indiana 47906 , United States.
Kyle E DentonDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy , Purdue University and Purdue University Center for Cancer Research , 575 Stadium Mall Drive , West Lafayette , Indiana 47906 , United States.
Kathryn F HobbsDepartment of Biochemistry, Carver College of Medicine , University of Iowa , 51 Newton Road , Iowa City , Iowa 52242 , United States.
Tyler WeaverDepartment of Biochemistry, Carver College of Medicine , University of Iowa , 51 Newton Road , Iowa City , Iowa 52242 , United States.
James M B McFarlaneDepartment of Chemistry , University of Victoria , Victoria V8W 3V6 , Canada.ORCID 0000-0002-2505-1408
Katelyn E ConnellyDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy , Purdue University and Purdue University Center for Cancer Research , 575 Stadium Mall Drive , West Lafayette , Indiana 47906 , United States.
Michael C GignacDepartment of Chemistry , University of Victoria , Victoria V8W 3V6 , Canada.
Natalia MilosevichDepartment of Chemistry , University of Victoria , Victoria V8W 3V6 , Canada.
Fraser HofDepartment of Chemistry , University of Victoria , Victoria V8W 3V6 , Canada.ORCID 0000-0003-4658-9132
Irina PaciDepartment of Chemistry , University of Victoria , Victoria V8W 3V6 , Canada.
Catherine A MusselmanDepartment of Biochemistry, Carver College of Medicine , University of Iowa , 51 Newton Road , Iowa City , Iowa 52242 , United States.ORCID 0000-0002-8356-7971
Emily C DykhuizenDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy , Purdue University and Purdue University Center for Cancer Research , 575 Stadium Mall Drive , West Lafayette , Indiana 47906 , United States.
Casey J KrusemarkDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy , Purdue University and Purdue University Center for Cancer Research , 575 Stadium Mall Drive , West Lafayette , Indiana 47906 , United States.ORCID 0000-0003-2964-3520
Purdue University West Lafayette · USUniversity of Victoria · CAUniversity of Iowa · US
Funding
Transgenic Mouse Core Facility Shared Resource (TMCF-SR)P30CA023168 · NCI · PURDUE UNIVERSITY WEST LAFAYETTE · PI John Tesmer · 1985 to 2026
$43.4MIndiana Clinical and Translational Sciences InstituteUL1TR001108 · NCATS · INDIANA UNIVERSITY INDIANAPOLIS · PI DENNE, SCOTT C., SHEKHAR, ANANTHA · 2013 to 2017
$23.3MMolecular mechanisms of histone signaling in a chromatin relevant contextR35GM128705 · NIGMS · UNIVERSITY OF IOWA · PI Catherine Anne Musselman · 2018 to 2026
$3.8MHarnessing the In Vitro Selection for Activity-based Proteomics and Chemical Probe DevelopmentR35GM128894 · NIGMS · PURDUE UNIVERSITY · PI Casey John Krusemark · 2018 to 2026
$3.2MThe tumor suppressive role of PBRM1, the bromodomain-containing subunit of the PBAF chromatin remodeling complexU01CA207532 · NCI · PURDUE UNIVERSITY · PI DYKHUIZEN, EMILY CARLA · 2017 to 2021
$1.7MDifferential Modulation of Cav1.2 and Cav1.3R21NS101535 · NINDS · PURDUE UNIVERSITY · PI HOCKERMAN, GREGORY HOWARD · 2017 to 2018
$409kNCATS NIH HHS UL1 TR001108NCI NIH HHS P30 CA023168NCI NIH HHS U01 CA207532NIGMS NIH HHS R35 GM128705NIGMS NIH HHS R35 GM128894NINDS NIH HHS R21 NS101535
Abstract
Polycomb repressive complex 1 (PRC1) is critical for mediating gene expression during development. Five chromobox (CBX) homolog proteins, CBX2, CBX4, CBX6, CBX7, and CBX8, are incorporated into PRC1 complexes, where they mediate targeting to trimethylated lysine 27 of histone H3 (H3K27me3)
Indexed as
Gene LibraryLigandsAmino Acid SequenceAntineoplastic AgentsCell Line, TumorCell Membrane PermeabilityCell ProliferationChromatinCloning, MolecularDNADrug DevelopmentEnzyme InhibitorsGene ExpressionHistonesHumansLigasesAntineoplastic AgentsCBX8 protein, humanChromatinDNAEnzyme InhibitorsHistonesLigandsLigasesLysinePolycomb Repressive Complex 1Recombinant Fusion Proteins
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.