Menghang Xia

Summary

Affiliation: National Institutes of Health
Country: USA

Publications

  1. pmc Identification of chemical compounds that induce HIF-1alpha activity
    Menghang Xia
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892, USA
    Toxicol Sci 112:153-63. 2009
  2. pmc Identification of repurposed small molecule drugs for chordoma therapy
    Menghang Xia
    NIH Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD, USA
    Cancer Biol Ther 14:638-47. 2013
  3. pmc Identification of quaternary ammonium compounds as potent inhibitors of hERG potassium channels
    Menghang Xia
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892 3370, USA
    Toxicol Appl Pharmacol 252:250-8. 2011
  4. pmc Identification of small molecule compounds that inhibit the HIF-1 signaling pathway
    Menghang Xia
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892 3370, USA
    Mol Cancer 8:117. 2009
  5. pmc Inhibition of morphine-induced cAMP overshoot: a cell-based assay model in a high-throughput format
    Menghang Xia
    NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
    Cell Mol Neurobiol 31:901-7. 2011
  6. pmc Application of a homogenous membrane potential assay to assess mitochondrial function
    Srilatha Sakamuru
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
    Physiol Genomics 44:495-503. 2012
  7. pmc Characterization of diversity in toxicity mechanism using in vitro cytotoxicity assays in quantitative high throughput screening
    Ruili Huang
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
    Chem Res Toxicol 21:659-67. 2008
  8. pmc Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors
    Amanda P Skoumbourdis
    NIH Chemical Genomics Center, National Human Genome Research Institute, NIH 9800 Medical Center Drive, MSC 3370 Bethesda, MD 20892 3370, USA
    Bioorg Med Chem Lett 19:3686-92. 2009
  9. pmc Profiling environmental chemicals for activity in the antioxidant response element signaling pathway using a high throughput screening approach
    Sunita J Shukla
    NIH Chemical Genomics Center, National Institutes of Health, Department of Health and Human Services, Rockville, Maryland, USA
    Environ Health Perspect 120:1150-6. 2012
  10. pmc A quantitative high-throughput screen for modulators of IL-6 signaling: a model for interrogating biological networks using chemical libraries
    Ronald L Johnson
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892, USA
    Mol Biosyst 5:1039-50. 2009

Collaborators

Detail Information

Publications33

  1. pmc Identification of chemical compounds that induce HIF-1alpha activity
    Menghang Xia
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892, USA
    Toxicol Sci 112:153-63. 2009
    ..Identification of environmental compounds having HIF-1alpha activation activity in cell-based assays may be useful for prioritizing chemicals for further testing as hypoxia-response inducers in vivo...
  2. pmc Identification of repurposed small molecule drugs for chordoma therapy
    Menghang Xia
    NIH Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD, USA
    Cancer Biol Ther 14:638-47. 2013
    ..Our results provide information useful for repurposing currently approved drugs for chordoma and potential approach of combination therapy. ..
  3. pmc Identification of quaternary ammonium compounds as potent inhibitors of hERG potassium channels
    Menghang Xia
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892 3370, USA
    Toxicol Appl Pharmacol 252:250-8. 2011
    ..Profiling environmental compound libraries for hERG channel inhibition provides information useful in prioritizing these compounds for cardiotoxicity assessment in vivo...
  4. pmc Identification of small molecule compounds that inhibit the HIF-1 signaling pathway
    Menghang Xia
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892 3370, USA
    Mol Cancer 8:117. 2009
    ..To identify small molecule inhibitors of the HIF-1 pathway, we have developed a cell-based reporter gene assay and screened a large compound library by using a quantitative high-throughput screening (qHTS) approach...
  5. pmc Inhibition of morphine-induced cAMP overshoot: a cell-based assay model in a high-throughput format
    Menghang Xia
    NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
    Cell Mol Neurobiol 31:901-7. 2011
    ..The qHTS approach we used in this study will be useful in identifying novel inhibitors of morphine induced addiction from a larger scale screening...
  6. pmc Application of a homogenous membrane potential assay to assess mitochondrial function
    Srilatha Sakamuru
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
    Physiol Genomics 44:495-503. 2012
    ..Our results demonstrate that this homogenous cell-based Mito-MPS assay can be used to evaluate the ability of large numbers of chemicals to decrease mitochondrial function...
  7. pmc Characterization of diversity in toxicity mechanism using in vitro cytotoxicity assays in quantitative high throughput screening
    Ruili Huang
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
    Chem Res Toxicol 21:659-67. 2008
    ..The performance of this clustering method is evaluated by comparing the clustering results against literature annotations of compound mechanisms...
  8. pmc Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors
    Amanda P Skoumbourdis
    NIH Chemical Genomics Center, National Human Genome Research Institute, NIH 9800 Medical Center Drive, MSC 3370 Bethesda, MD 20892 3370, USA
    Bioorg Med Chem Lett 19:3686-92. 2009
    ..Finally, docking studies with selective ligands (including 10 and 18) were undertaken to better understand this chemotypes ability to bind and inhibit PDE4 selectively...
  9. pmc Profiling environmental chemicals for activity in the antioxidant response element signaling pathway using a high throughput screening approach
    Sunita J Shukla
    NIH Chemical Genomics Center, National Institutes of Health, Department of Health and Human Services, Rockville, Maryland, USA
    Environ Health Perspect 120:1150-6. 2012
    ..Thus, assays that detect the up-regulation of this pathway could be useful for identifying chemicals that induce oxidative stress...
  10. pmc A quantitative high-throughput screen for modulators of IL-6 signaling: a model for interrogating biological networks using chemical libraries
    Ronald L Johnson
    NIH Chemical Genomics Center, National Institutes of Health, Bethesda, MD 20892, USA
    Mol Biosyst 5:1039-50. 2009
    ..Small molecules within these series will make useful tool compounds to investigate IL-6 signaling mediated by JAK-STAT activation...
  11. pmc Weighted feature significance: a simple, interpretable model of compound toxicity based on the statistical enrichment of structural features
    Ruili Huang
    Department of Health and Human Services, NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
    Toxicol Sci 112:385-93. 2009
    ..The new algorithm has the important advantages of simplicity, power, interpretability, and ease of implementation...
  12. pmc Identification of compounds that potentiate CREB signaling as possible enhancers of long-term memory
    Menghang Xia
    NIH Chemical Genomics Center, National Heart, Lung, and Blood Institute, National Institutes of Health, Bethesda, MD 20892, USA
    Proc Natl Acad Sci U S A 106:2412-7. 2009
    ..qHTS followed by interrogation of pathway targets is an efficient paradigm for lead generation for chemical genomics and drug development...
  13. pmc A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-a-go-go-related gene channel
    Steven A Titus
    NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
    Anal Biochem 394:30-8. 2009
    ..Our findings indicate that this thallium flux assay can be used as an alternative method to profile large-volume compound libraries for compound activity on the hERG channel...
  14. pmc A bioluminescent cytotoxicity assay for assessment of membrane integrity using a proteolytic biomarker
    Ming Hsuang Cho
    NIH Chemical Genomics Center, National Institutes of Health, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892 3370, USA
    Toxicol In Vitro 22:1099-106. 2008
    ..This cytotoxicity assay, combined with the qHTS platform, allowed us to quickly and efficiently evaluate compound toxicities related to cell membrane integrity...
  15. pmc Compound cytotoxicity profiling using quantitative high-throughput screening
    Menghang Xia
    NIH Chemical Genomics Center, National Institutes of Health, Department of Health and Human Services, Bethesda, Maryland 20892 3370, USA
    Environ Health Perspect 116:284-91. 2008
    ..Such methods can be relatively expensive, low-throughput, and associated with pain suffered by the treated animals. In addition, differences in species biology may confound extrapolation to human health effects...
  16. pmc Identification of a potent new chemotype for the selective inhibition of PDE4
    Amanda P Skoumbourdis
    NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Drive, MSC 3370, Bethesda, MD 20892 3370, USA
    Bioorg Med Chem Lett 18:1297-303. 2008
    ..Synthesis, structure-activity relationships, and the selectivity of a highly potent analogue against related phosphodiesterase isoforms are presented...
  17. pmc The Tox21 robotic platform for the assessment of environmental chemicals - from vision to reality
    Matias S Attene-Ramos
    NIH Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, MD 20850, USA
    Drug Discov Today 18:716-23. 2013
    ..In this article, we describe the Tox21 screening process, compound library preparation, data processing, and robotic system validation. ..
  18. pmc Identification of clinically used drugs that activate pregnane X receptors
    Sunita J Shukla
    National Institutes of Health Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, USA
    Drug Metab Dispos 39:151-9. 2011
    ....
  19. pmc Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors
    Wenwei Huang
    NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Dr, Rockville, MD 20850, USA
    Bioorg Med Chem Lett 21:5239-43. 2011
    ..In this Letter, we describe an efficient one-pot sequential reaction for the synthesis of quinazolin-4-one 1 analogues. The structure-activity relationship (SAR) study led to the 5-fold more potent analogue, 16...
  20. pmc Are hERG channel blockers also phospholipidosis inducers?
    Hongmao Sun
    National Center for Advancing Translational Sciences, National Institutes of Health NIH, 9800 Medical Center Drive, Bethesda, Rockville, MD 20892, USA
    Bioorg Med Chem Lett 23:4587-90. 2013
    ..In addition, a positively charged hERG channel blocker will most likely induce PLD, while a steroid PLD inducer is less likely a hERG channel blocker. ..
  21. doi request reprint Systematic study of mitochondrial toxicity of environmental chemicals using quantitative high throughput screening
    Matias S Attene-Ramos
    National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, United States
    Chem Res Toxicol 26:1323-32. 2013
    ..This comprehensive approach allows for the evaluation of thousands of environmental chemicals for mitochondrial toxicity and identification of possible MOAs. ..
  22. pmc Chemical genomics profiling of environmental chemical modulation of human nuclear receptors
    Ruili Huang
    National Institutes of Health Chemical Genomics Center, National Institutes of Health, Department of Health and Human Services, Bethesda, Maryland 20892 3370, USA
    Environ Health Perspect 119:1142-8. 2011
    ....
  23. pmc Phosphodiesterase 4 inhibitors enhance sexual pleasure-seeking activity in rodents
    Peixiong Yuan
    Biomarker Laboratory, National Institute of Mental Health, Mood and Anxiety Disorders Program, National Institutes of Health, Bethesda, MD 20892, USA
    Pharmacol Biochem Behav 98:349-55. 2011
    ..The results suggest that PDE4 may be a plausible contributor to the sexual pleasure-seeking deficits seen in depressed patients; inhibiting PDE4 may restore these deficits...
  24. pmc Identification of known drugs that act as inhibitors of NF-kappaB signaling and their mechanism of action
    Susanne C Miller
    NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
    Biochem Pharmacol 79:1272-80. 2010
    ..Comprehensive profiling of approved drugs provides insight into their molecular mechanisms, thus providing a basis for drug repurposing...
  25. pmc The pilot phase of the NIH Chemical Genomics Center
    Craig J Thomas
    NIH Chemical Genomics Center, NHGRI, National Institutes of Health, 9800 Medical Center Drive, Building B, Room 3005, MSC 3370, Bethesda, MD 20892 3370, USA
    Curr Top Med Chem 9:1181-93. 2009
    ....
  26. pmc High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death
    Jennifer T Fox
    Genome Instability Section, Genetics and Molecular Biology Branch, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
    Proc Natl Acad Sci U S A 109:5423-8. 2012
    ..Furthermore, resveratrol and genistein killed multidrug-resistant cancer cells. We therefore propose that resveratrol, genistein, and baicalein are attractive candidates for improved chemotherapeutic agents...
  27. pmc Paradigm shift in toxicity testing and modeling
    Hongmao Sun
    Department of Health and Human Services, NIH Chemical Genomics Center, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
    AAPS J 14:473-80. 2012
    ..It is perceivable that new in silico toxicity models based on high-quality qHTS data will achieve unprecedented reliability and robustness, thus becoming a valuable tool for risk assessment and drug discovery...
  28. pmc The future of toxicity testing: a focus on in vitro methods using a quantitative high-throughput screening platform
    Sunita J Shukla
    NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892 3370, USA
    Drug Discov Today 15:997-1007. 2010
    ..Here, we describe the Tox21 collaboration, qHTS-based compound testing and the various Tox21 screening assays that have been validated and tested at the NCGC to date...
  29. doi request reprint Detection of phospholipidosis induction: a cell-based assay in high-throughput and high-content format
    Sampada A Shahane
    1National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD, USA
    J Biomol Screen 19:66-76. 2014
    ..These results demonstrate that this assay can be used to evaluate and profile large numbers of chemicals for drug-induced phospholipidosis. ..
  30. pmc Structure based model for the prediction of phospholipidosis induction potential of small molecules
    Hongmao Sun
    National Institutes of Health NIH Chemical Genomics Center, NIH, Bethesda, Maryland 20892, United States
    J Chem Inf Model 52:1798-805. 2012
    ..90 in predicting the remaining two-thirds of the compounds constituting the test set, as measured by the area under the receiver operator characteristic curve (AUC-ROC). ..
  31. pmc Predictive models for cytochrome p450 isozymes based on quantitative high throughput screening data
    Hongmao Sun
    National Institutes of Health, Chemical Genomics Center, NIH, Bethesda, Maryland 20892, United States
    J Chem Inf Model 51:2474-81. 2011
    ..These models can be useful in prioritizing compounds in a drug discovery pipeline or recognizing the toxic potential of environmental chemicals...
  32. ncbi request reprint High-throughput screening assays for the identification of chemical probes
    James Inglese
    US National Institutes of Health Chemical Genomics Center, National Institutes of Health, 9800 Medical Center Drive, Bethesda, Maryland 20892 3370, USA
    Nat Chem Biol 3:466-79. 2007
    ..We conclude with special considerations for configuring sensitive, robust, informative and economically feasible HTS assays...
  33. pmc Two High Throughput Screen Assays for Measurement of TNF-α in THP-1 Cells
    Kristin P Leister
    NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
    Curr Chem Genomics 5:21-9. 2011
    ..We also identified several novel inhibitors of TNF-α, such as BTO-1, CCG-2046, ellipticine, and PD 169316. The results demonstrated that both homogeneous TNF-α assays are robust and suitable for high throughput screening...