Structural Genomics Consortium,
Department of Pharmacology and Toxicology,
Pharmacology and Toxicology and Structural Genomics Consortium
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Analysis of Myc bound loci identified by CpG island arrays shows that Max is essential for Myc-dependent repression.
Current biology : CB May, 2003 | Pubmed ID: 12747840
c-Myc represses the proximal promoters of GADD45a and GADD153 by a post-RNA polymerase II recruitment mechanism.
Oncogene , | Pubmed ID: 15021909
Cloning and characterization of teneurin C-terminus associated peptide (TCAP)-3 from the hypothalamus of an adult rainbow trout (Oncorhynchus mykiss).
General and comparative endocrinology , | Pubmed ID: 15158132
Promoter-binding and repression of PDGFRB by c-Myc are separable activities.
Nucleic acids research , | Pubmed ID: 15226411
Teneurin proteins possess a carboxy terminal sequence with neuromodulatory activity.
Brain research. Molecular brain research , | Pubmed ID: 15710242
Cancer therapeutics: targeting the dark side of Myc.
European journal of cancer (Oxford, England : 1990) , | Pubmed ID: 16243519
The c-Myc oncogene directly induces the H19 noncoding RNA by allele-specific binding to potentiate tumorigenesis.
Cancer research , | Pubmed ID: 16707459
Integrin alpha 11 regulates IGF2 expression in fibroblasts to enhance tumorigenicity of human non-small-cell lung cancer cells.
Proceedings of the National Academy of Sciences of the United States of America , | Pubmed ID: 17600088
Teneurin carboxy (C)-terminal associated peptide-1 inhibits alkalosis-associated necrotic neuronal death by stimulating superoxide dismutase and catalase activity in immortalized mouse hypothalamic cells.
Brain research , | Pubmed ID: 17900539
CUL7 is a novel antiapoptotic oncogene.
Cancer research Oct, 2007 | Pubmed ID: 17942889
Evolution of complementary peptide systems: teneurin C-terminal-associated peptides and corticotropin-releasing factor superfamilies.
Annals of the New York Academy of Sciences , | Pubmed ID: 19456342
Characterization of a corticotropin-releasing factor (CRF)/diuretic hormone-like peptide from tunicates: insight into the origins of the vertebrate CRF family.
General and comparative endocrinology , | Pubmed ID: 19646444
A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.
Nature chemical biology Aug, 2011 | Pubmed ID: 21743462
Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.
Journal of medicinal chemistry Sep, 2011 | Pubmed ID: 21780790
Histone recognition and large-scale structural analysis of the human bromodomain family.
Cell , | Pubmed ID: 22464331
Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5.
The Biochemical journal Jan, 2013 | Pubmed ID: 22989411
Association of UHRF1 with methylated H3K9 directs the maintenance of DNA methylation.
Nature structural & molecular biology Nov, 2012 | Pubmed ID: 23022729
C-terminal processing of the teneurin proteins: independent actions of a teneurin C-terminal associated peptide in hippocampal cells.
Molecular and cellular neurosciences , | Pubmed ID: 23026563
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Nature communications , 2012 | Pubmed ID: 23250418
Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain.
Nature chemical biology Jan, 2013 | Pubmed ID: 23292653
Systems approaches to genomic and epigenetic inter-regulation of peptide hormones in stress and reproduction.
Progress in biophysics and molecular biology , | Pubmed ID: 23500148
An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.
ACS chemical biology , 2013 | Pubmed ID: 23614352
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
Journal of medicinal chemistry Nov, 2013 | Pubmed ID: 24102134
A chemical tool for in vitro and in vivo precipitation of lysine methyltransferase G9a.
ChemMedChem , | Pubmed ID: 24443078
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Proceedings of the National Academy of Sciences of the United States of America Sep, 2014 | Pubmed ID: 25136132
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
LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2.
The Journal of biological chemistry May, 2015 | Pubmed ID: 25825497
Discovery of a Dual PRMT5-PRMT7 Inhibitor.
ACS medicinal chemistry letters , | Pubmed ID: 25893041
Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia.
Nature chemical biology , | Pubmed ID: 26167872
Gain-of-function p53 mutants co-opt chromatin pathways to drive cancer growth.
Nature , | Pubmed ID: 26331536
A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.
ACS chemical biology Mar, 2016 | Pubmed ID: 26598975
MLL5 Orchestrates a Cancer Self-Renewal State by Repressing the Histone Variant H3.3 and Globally Reorganizing Chromatin.
Cancer cell , | Pubmed ID: 26626085
Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor.
Journal of medicinal chemistry , | Pubmed ID: 26824386
Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2.
Journal of medicinal chemistry , | Pubmed ID: 27075367
An Integrative Proteomic Approach Identifies Novel Cellular SMYD2 Substrates.
Journal of proteome research , | Pubmed ID: 27163177
Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening.
Journal of medicinal chemistry , | Pubmed ID: 27390919
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
Integrated (epi)-Genomic Analyses Identify Subgroup-Specific Therapeutic Targets in CNS Rhabdoid Tumors.
Cancer cell , | Pubmed ID: 27960086
The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity.
Nature chemical biology , | Pubmed ID: 28114273
The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.
Nature chemical biology , | Pubmed ID: 28135237
Targeting human SET1/MLL family of proteins.
Protein science : a publication of the Protein Society , | Pubmed ID: 28160335
Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors.
Nature communications , | Pubmed ID: 29142305
Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).
Journal of medicinal chemistry Feb, 2018 | Pubmed ID: 29244490
TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma.
Oncotarget , | Pubmed ID: 29719619
Mammary molecular portraits reveal lineage-specific features and progenitor cell vulnerabilities.
The Journal of cell biology , | Pubmed ID: 29921600
LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity.
ACS medicinal chemistry letters , | Pubmed ID: 30034588
Characterization of inv(3) cell line OCI-AML-20 with stroma-dependent CD34 expression.
Experimental hematology , | Pubmed ID: 30352278
Direct interaction between the PRDM3 and PRDM16 tumor suppressors and the NuRD chromatin remodeling complex.
Nucleic acids research , | Pubmed ID: 30462309
A chemical biology toolbox to study protein methyltransferases and epigenetic signaling.
Nature communications , | Pubmed ID: 30604761
Teneurin C-Terminal Associated Peptide (TCAP)-1 and Latrophilin Interaction in HEK293 Cells: Evidence for Modulation of Intercellular Adhesion.
Frontiers in endocrinology , | Pubmed ID: 30774623
Targeting bivalency de-represses Indian Hedgehog and inhibits self-renewal of colorectal cancer-initiating cells.
Nature communications , | Pubmed ID: 30926792
Targeting protein methylation: from chemical tools to precision medicines.
Cellular and molecular life sciences : CMLS , | Pubmed ID: 31104094
Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1).
Journal of medicinal chemistry , | Pubmed ID: 31260300
Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3.
Nature chemical biology , | Pubmed ID: 31285596
A C19MC-LIN28A-MYCN Oncogenic Circuit Driven by Hijacked Super-enhancers Is a Distinct Therapeutic Vulnerability in ETMRs: A Lethal Brain Tumor.
Cancer cell , | Pubmed ID: 31287992
Therapeutic Targeting of RNA Splicing Catalysis through Inhibition of Protein Arginine Methylation.
Cancer cell , | Pubmed ID: 31408619
Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3-9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase.
Journal of medicinal chemistry , | Pubmed ID: 31415173
SETD7 at the heart of chromatin factor interplay.
Stem cell investigation , | Pubmed ID: 31559307
Synthetic Peptides as Therapeutic Agents: Lessons Learned From Evolutionary Ancient Peptides and Their Transit Across Blood-Brain Barriers.
Frontiers in endocrinology , | Pubmed ID: 31781029
Discovery of a chemical probe for PRDM9.
Nature communications , | Pubmed ID: 31848333
Telomere dysfunction cooperates with epigenetic alterations to impair murine embryonic stem cell fate commitment.
eLife , | Pubmed ID: 32297856
Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor.
Journal of medicinal chemistry , | Pubmed ID: 32367723
Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response.
Nature communications , | Pubmed ID: 32409666
Author Correction: Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response.
Nature communications , | Pubmed ID: 32457299
Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2.
Journal of medicinal chemistry 02, 2021 | Pubmed ID: 33522809
PRMT5 inhibition disrupts splicing and stemness in glioblastoma.
Nature communications 02, 2021 | Pubmed ID: 33579912
A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6.
Journal of medicinal chemistry 04, 2021 | Pubmed ID: 33591753
Protein arginine methylation: from enigmatic functions to therapeutic targeting.
Nature reviews. Drug discovery 07, 2021 | Pubmed ID: 33742187
Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders.
Journal of medicinal chemistry May, 2021 | Pubmed ID: 33980013
Discovery of the SMYD3 Inhibitor BAY-6035 Using Thermal Shift Assay (TSA)-Based High-Throughput Screening.
SLAS discovery : advancing life sciences R & D Jun, 2021 | Pubmed ID: 34154424
Development of LM98, a Small-Molecule TEAD Inhibitor Derived from Flufenamic Acid.
ChemMedChem Jun, 2021 | Pubmed ID: 34164919
Structure and Function of Protein Arginine Methyltransferase PRMT7.
Life (Basel, Switzerland) Jul, 2021 | Pubmed ID: 34440512
A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization.
Nature chemical biology Jan, 2022 | Pubmed ID: 34782742
PRMT5 regulates ATF4 transcript splicing and oxidative stress response.
Redox biology May, 2022 | Pubmed ID: 35305370
PRMT7 ablation stimulates anti-tumor immunity and sensitizes melanoma to immune checkpoint blockade.
Cell reports Mar, 2022 | Pubmed ID: 35354055
Validating Small Molecule Chemical Probes for Biological Discovery.
Annual review of biochemistry Jun, 2022 | Pubmed ID: 35363509
PRMT inhibition induces a viral mimicry response in triple-negative breast cancer.
Nature chemical biology Aug, 2022 | Pubmed ID: 35578032
Chemical biology and pharmacology of histone lysine methylation inhibitors.
Biochimica et biophysica acta. Gene regulatory mechanisms Aug, 2022 | Pubmed ID: 35753676
Enzymatic nucleosome acetylation selectively affects activity of histone methyltransferases in vitro.
Biochimica et biophysica acta. Gene regulatory mechanisms Jul, 2022 | Pubmed ID: 35907431
Combinatorial Anticancer Drug Screen Identifies Off-Target Effects of Epigenetic Chemical Probes.
ACS chemical biology Oct, 2022 | Pubmed ID: 36084291
Distal extracellular teneurin region (teneurin C-terminal associated peptide; TCAP) possesses independent intracellular calcium regulating actions, : A potential antagonist of corticotropin-releasing factor (CRF).
Biochemistry and biophysics reports Dec, 2022 | Pubmed ID: 36467544
Skeletal muscle metabolism and contraction performance regulation by teneurin C-terminal-associated peptide-1.
Frontiers in physiology , 2022 | Pubmed ID: 36523555
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