A5034141988- Epigenetics and DNA Methylation
- Cancer-related gene regulation
- Histone Deacetylase Inhibitors Research
- RNA modifications and cancer
- Sphingolipid Metabolism and Signaling
- Protein Degradation and Inhibitors
- Genomics and Chromatin Dynamics
- Ferroptosis and cancer prognosis
- Ubiquitin and proteasome pathways
- Erythrocyte Function and Pathophysiology
- Antibiotic Resistance in Bacteria
- Multiple Myeloma Research and Treatments
- Antibiotics Pharmacokinetics and Efficacy
- Acute Myeloid Leukemia Research
- Zebrafish Biomedical Research Applications
- Cancer-related molecular mechanisms research
- Genetic Syndromes and Imprinting
- Bioactive Natural Diterpenoids Research
- Peptidase Inhibition and Analysis
- Chronic Myeloid Leukemia Treatments
- Autophagy in Disease and Therapy
- Cancer, Hypoxia, and Metabolism
- PI3K/AKT/mTOR signaling in cancer
- Research on Leishmaniasis Studies
- Invertebrate Immune Response Mechanisms
Georgia State University
2015-2019
Shanghai Jiao Tong University
2010-2016
Ruijin Hospital
2015
Shanghai Institute of Hematology
2010-2014
Shanghai Institutes for Biological Sciences
2012
Metabolic reprogramming of cancer cells is essential for tumorigenesis in which pyruvate kinase M2 (PKM2), the low activity isoform kinase, plays a critical role. Herein, we describe identification nature-product-derived micheliolide (MCL) that selectively activates PKM2 through covalent binding at residue cysteine424 (C424), not contained PKM1. This interaction promotes more tetramer formation, inhibits lysine433 (K433) acetylation, and influences translocation into nucleus. In addition,...
Oridonin treats AML by generating a truncated version of the AML1-ETO oncoprotein that functions as tumor suppressor.
Arsenic, a curative agent for acute promyelocytic leukemia, induces cell apoptosis and degradation of BCR-ABL in chronic myelogenous leukemia (CML). We demonstrated that ubiquitination was mediated by c-CBL, RING-type E3 ligase also shown to be involved many other receptor/protein tyrosine kinases. Our data showed c-CBL protein considerably up-regulated arsenic sulfide (As(4)S(4)). Interestingly, directly bound the RING finger domain inhibit its self-ubiquitination/degradation without...
Protein arginine methyltransferases (PRMTs) are proved to play vital roles in chromatin remodeling, RNA metabolism, and signal transduction. Aberrant regulation of PRMT activity is associated with various pathological states such as cancer cardiovascular disorders. Development application small molecule inhibitors will provide new avenues for therapeutic discovery. The combination pharmacophore-based virtual screening methods radioactive methylation assays provided six hits identified...
The New Delhi Metallo-β-lactamase (NDM-1) was first reported in 2009 a Swedish patient. A recent study that Klebsiella pneumonia NDM-1 positive strain or Escherichia coli highly resistant to all antibiotics tested except tigecycline and colistin. These can no longer be relied on treat infections therefore, now becomes potentially major global health threat. In this study, we performed modeling studies obtain its 3D structure NDM-1/antibiotics complex. It revealed the hydrolytic mechanisms...
The M2 subtype Acute Myeloid Leukemia (AML-M2) with t(8;21) represents an unmet challenge because of poor clinical outcomes in a sizable portion patients. In this study,we report that FTY720 (Fingolimod), sphingosine analogue and FDA approved drug for treating multiple sclerosis, shows antitumorigenic activity against the Kasumi-1 cell line, xenograft mouse models leukemic blasts isolated from AML-M2 patients translocation. Primary investigation indicated caused apoptosis through caspases...
Lysine-specific demethylase 1 (LSD1), the first identified histone demethylase, is a flavin-dependent amine oxidase which specifically demethylates mono- or dimethylated H3K4 and H3K9 via redox process. It participates in broad spectrum of biological processes high importance cell proliferation, adipogenesis, spermatogenesis, chromosome segregation embryonic development. To date, as potential drug target for discovering anti-tumor drugs, medical significance LSD1 has been greatly...
Aberrant enzymatic activities or expression profiles of epigenetic regulations are therapeutic targets for cancers. Among these, histone 3 lysine 9 methylation (H3K9Me2) and global de-acetylation on proteins associated with multiple cancer phenotypes including leukemia, prostatic carcinoma, hepatocellular carcinoma pulmonary carcinoma. Here, we report the discovery first small molecule capable acting as a dual inhibitor targeting both G9a HDAC. Our structure based design, synthesis,...
Lapatinib is a small molecule inhibitor of EGFR (HER1) and ERBB2 (HER2) receptors, which used for treatment advanced or metastatic breast cancer. To find the drug resistance mechanisms EGFR/ERBB2 positive tumors, we analyzed possible effects lncRNAs. In this study, using CCLE (Cancer Cell Line Encyclopedia) database, explored relationship between lncRNAs sensitivity/resistance, then validated those findings through in vitro experiments. We found that expression activation ERBB pathway was...
Histone methylation represents one of the most critical epigenetic events in DNA function regulation eukaryotic organisms. Classic molecular biology and genetics tools provide significant knowledge about mechanisms physiological roles histone methyltransferases demethylases various cellular processes. In addition to this stream line, development application chemistry chemistry-related techniques are increasingly involved biological study, offer information otherwise difficult obtain by...