Chemical Biology and Drug Discovery,
Pharmacological Sciences and Oncological Sciences,
Chemical Biology and Drug Discovery, Pharmacological Sciences and Oncological Sciences
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Development of a S-adenosylmethionine analog that intrudes the RNA-cap binding site of Zika methyltransferase.
Scientific reports May, 2017 | Pubmed ID: 28487506
Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia.
Blood Jan, 2015 | Pubmed ID: 25395428
Selective inhibitors of protein methyltransferases.
Journal of medicinal chemistry Feb, 2015 | Pubmed ID: 25406853
Chemical probes of histone lysine methyltransferases.
ACS chemical biology Jan, 2015 | Pubmed ID: 25423077
A chromatin activity-based chemoproteomic approach reveals a transcriptional repressome for gene-specific silencing.
Nature communications Dec, 2014 | Pubmed ID: 25502336
EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells.
Cancer biology & therapy , 2014 | Pubmed ID: 25535899
Structure-activity relationship studies of SETD8 inhibitors.
MedChemComm Dec, 2014 | Pubmed ID: 25554733
The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs.
ACS chemical neuroscience Mar, 2015 | Pubmed ID: 25587888
A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
Angewandte Chemie (International ed. in English) Apr, 2015 | Pubmed ID: 25728001
Targeting EZH2 and PRC2 dependence as novel anticancer therapy.
Experimental hematology Aug, 2015 | Pubmed ID: 26027790
Non-canonical Bromodomain within DNA-PKcs Promotes DNA Damage Response and Radioresistance through Recognizing an IR-Induced Acetyl-Lysine on H2AX.
Chemistry & biology Jul, 2015 | Pubmed ID: 26119999
Effects of β-Arrestin-Biased Dopamine D2 Receptor Ligands on Schizophrenia-Like Behavior in Hypoglutamatergic Mice.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology Feb, 2016 | Pubmed ID: 26129680
The promise and peril of chemical probes.
Nature chemical biology Aug, 2015 | Pubmed ID: 26196764
A Role for Widely Interspaced Zinc Finger (WIZ) in Retention of the G9a Methyltransferase on Chromatin.
The Journal of biological chemistry Oct, 2015 | Pubmed ID: 26338712
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.
ACS chemical biology Mar, 2016 | Pubmed ID: 26598975
Genome-wide profiling of histone H3 lysine 27 and lysine 4 trimethylation in multiple myeloma reveals the importance of Polycomb gene targeting and highlights EZH2 as a potential therapeutic target.
Oncotarget Feb, 2016 | Pubmed ID: 26755663
Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform.
Nucleic acids research 05, 2016 | Pubmed ID: 26893353
Novel Therapeutics Targeting Epigenetics: New Molecules, New Methods.
ACS medicinal chemistry letters Feb, 2016 | Pubmed ID: 26985299
Topoisomerase 1 inhibition suppresses inflammatory genes and protects from death by inflammation.
Science (New York, N.Y.) May, 2016 | Pubmed ID: 27127234
Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors.
Journal of medicinal chemistry 08, 2016 | Pubmed ID: 27468126
Non-Substrate Based, Small Molecule Inhibitors of the Human Isoprenylcysteine Carboxyl Methyltransferase.
MedChemComm May, 2016 | Pubmed ID: 27547295
Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.
Journal of medicinal chemistry 10, 2016 | Pubmed ID: 27584694
Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase.
Journal of medicinal chemistry 11, 2016 | Pubmed ID: 27804297
Discovery of G Protein-Biased D2 Dopamine Receptor Partial Agonists.
Journal of medicinal chemistry 12, 2016 | Pubmed ID: 27805392
Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties.
Proceedings of the National Academy of Sciences of the United States of America 12, 2016 | Pubmed ID: 27911814
Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader-Willi syndrome.
Nature medicine Feb, 2017 | Pubmed ID: 28024084
EZH2 inhibition in multiple myeloma downregulates myeloma associated oncogenes and upregulates microRNAs with potential tumor suppressor functions.
Oncotarget Feb, 2017 | Pubmed ID: 28052011
Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma.
Cancer cell 01, 2017 | Pubmed ID: 28073004
Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase.
Journal of medicinal chemistry Mar, 2017 | Pubmed ID: 28135087
Hsp90 inhibition destabilizes Ezh2 protein in alloreactive T cells and reduces graft-versus-host disease in mice.
Blood 05, 2017 | Pubmed ID: 28246193
An Oral Selective Alpha-1A Adrenergic Receptor Agonist Prevents Doxorubicin Cardiotoxicity.
JACC. Basic to translational science Feb, 2017 | Pubmed ID: 28286875
In silico design of novel probes for the atypical opioid receptor MRGPRX2.
Nature chemical biology 05, 2017 | Pubmed ID: 28288109
Inhibitors of Protein Methyltransferases and Demethylases.
Chemical reviews Feb, 2018 | Pubmed ID: 28338320
Dual Inhibition of EZH2 and EZH1 Sensitizes PRC2-Dependent Tumors to Proteasome Inhibition.
Clinical cancer research : an official journal of the American Association for Cancer Research Aug, 2017 | Pubmed ID: 28490465
Recent progress in developing selective inhibitors of protein methyltransferases.
Current opinion in chemical biology Aug, 2017 | Pubmed ID: 28662389
Structure-activity relationship studies of G9a-like protein (GLP) inhibitors.
Bioorganic & medicinal chemistry 08, 2017 | Pubmed ID: 28662962
Report and Application of a Tool Compound Data Set.
Journal of chemical information and modeling 11, 2017 | Pubmed ID: 29035535
Targeted Gene Repression Using Novel Bifunctional Molecules to Harness Endogenous Histone Deacetylation Activity.
ACS synthetic biology 01, 2018 | Pubmed ID: 29073761
Structure-inspired design of β-arrestin-biased ligands for aminergic GPCRs.
Nature chemical biology Feb, 2018 | Pubmed ID: 29227473
VE-Cadherin-Mediated Epigenetic Regulation of Endothelial Gene Expression.
Circulation research Jan, 2018 | Pubmed ID: 29233846
Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).
Journal of medicinal chemistry Feb, 2018 | Pubmed ID: 29244490
The polycomb group protein BMI-1 inhibitor PTC-209 is a potent anti-myeloma agent alone or in combination with epigenetic inhibitors targeting EZH2 and the BET bromodomains.
Oncotarget Nov, 2017 | Pubmed ID: 29262596
Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT).
Journal of medicinal chemistry Feb, 2018 | Pubmed ID: 29320176
Inhibition of the G9a/GLP histone methyltransferase complex modulates anxiety-related behavior in mice.
Acta pharmacologica Sinica May, 2018 | Pubmed ID: 29417943
Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK).
European journal of medicinal chemistry May, 2018 | Pubmed ID: 29627725
Structural determinants of 5-HT receptor activation and biased agonism.
Nature structural & molecular biology Sep, 2018 | Pubmed ID: 30127358
Influenza virus infection causes global RNAPII termination defects.
Nature structural & molecular biology Sep, 2018 | Pubmed ID: 30177761
1Chemical Biology and Medicinal Chemistry, Center for Integrative Chemical Biology and Drug Discovery, Curriculum in Genetics and Molecular Biology, University of North Carolina,
2College of Arts and Sciences, Chemical Biology and Medicinal Chemistry, Center for Integrative Chemical Biology and Drug Discovery, University of North Carolina,
3Chemical Biology and Drug Discovery, Pharmacological Sciences and Oncological Sciences, Icahn School of Medicine at Mount Sinai,
4Chemical Biology and Medicinal Chemistry, Center for Integrative Chemical Biology and Drug Discovery, Curriculum in Genetics and Molecular Biology, Lineberger Comprehensive Cancer Center, University of North Carolina