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An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.
EZH2 or EZH1 is the catalytic subunit of the polycomb repressive complex 2 that catalyzes methylation of histone H3 lysine 27 (H3K27). The trimethylation of H3K27 (H3K27me3) is a transcriptionallyExpand
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Discovery of β-Arrestin–Biased Dopamine D2 Ligands for Probing Signal Transduction Pathways Essential for Antipsychotic Efficacy
  • J. Allen, J. Yost, +16 authors J. Jin
  • Biology, Medicine
  • Proceedings of the National Academy of Sciences
  • 24 October 2011
Elucidating the key signal transduction pathways essential for both antipsychotic efficacy and side-effect profiles is essential for developing safer and more effective therapies. Recent work hasExpand
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Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
Among epigenetic "writers", "readers", and "erasers", the lysine methyltransferases G9a and GLP, which catalyze mono- and dimethylation of histone H3 lysine 9 (H3K9me2) and nonhistone proteins, haveExpand
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Inhibitors of Protein Methyltransferases and Demethylases
Post-translational modifications of histones by protein methyltransferases (PMTs) and histone demethylases (KDMs) play an important role in the regulation of gene expression and transcription and areExpand
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Topoisomerase 1 inhibition suppresses inflammatory genes and protects from death by inflammation
Unwinding DNA and unleasing inflammation Fighting infections often comes with collateral damage, which sometimes can be deadly. For instance, in septic shock, the overwhelming release of inflammatoryExpand
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Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.
Protein lysine methyltransferase G9a plays key roles in the transcriptional repression of a variety of genes via dimethylation of lysine 9 on histone H3 (H3K9me2) of chromatin as well asExpand
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Essential role for TrpC5-containing extracellular vesicles in breast cancer with chemotherapeutic resistance
  • X. Ma, Z. Chen, +24 authors X. Yao
  • Biology, Medicine
  • Proceedings of the National Academy of Sciences
  • 14 April 2014
Significance A critical challenge for chemotherapy is development of chemoresistance, but underlying molecular mechanisms remain unclear. In this study, we found that drug-resistantExpand
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Transient receptor potential channel TRPC5 is essential for P-glycoprotein induction in drug-resistant cancer cells
  • X. Ma, Yanfei Cai, +11 authors X. Yao
  • Biology, Medicine
  • Proceedings of the National Academy of Sciences
  • 17 September 2012
An attractive strategy to overcome multidrug resistance in cancer chemotherapy is to suppress P-glycoprotein (P-gp), which is a pump overproduced in cancer cells to remove cytotoxic drugs from cells.Expand
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Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice.
Adenosine A(1) receptor (A(1)AR) agonists have antinociceptive effects in multiple preclinical models of acute and chronic pain. Although numerous A(1)AR agonists have been developed, clinicalExpand
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Hsp90 inhibition destabilizes Ezh2 protein in alloreactive T cells and reduces graft-versus-host disease in mice.
Modulating T-cell alloreactivity has been a main strategy to reduce graft-versus-host disease (GVHD), a life-threatening complication after allogeneic hematopoietic stem-cell transplantation (HSCT).Expand
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