Research Topics
Species | Menghang XiaSummaryAffiliation: National Institutes of Health Country: USA Publications
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Detail Information
Publications
Identification of chemical compounds that induce HIF-1alpha activityMenghang 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...- Identification of quaternary ammonium compounds as potent inhibitors of hERG potassium channelsMenghang 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... - Inhibition of morphine-induced cAMP overshoot: a cell-based assay model in a high-throughput formatMenghang 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... - Identification of small molecule compounds that inhibit the HIF-1 signaling pathwayMenghang 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... - Application of a homogenous membrane potential assay to assess mitochondrial functionSrilatha 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... - Characterization of diversity in toxicity mechanism using in vitro cytotoxicity assays in quantitative high throughput screeningRuili 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... - Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitorsAmanda 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... - Weighted feature significance: a simple, interpretable model of compound toxicity based on the statistical enrichment of structural featuresRuili 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... - Identification of compounds that potentiate CREB signaling as possible enhancers of long-term memoryMenghang 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... - A quantitative high-throughput screen for modulators of IL-6 signaling: a model for interrogating biological networks using chemical librariesRonald 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... - A new homogeneous high-throughput screening assay for profiling compound activity on the human ether-a-go-go-related gene channelSteven 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... - A bioluminescent cytotoxicity assay for assessment of membrane integrity using a proteolytic biomarkerMing 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... - Compound cytotoxicity profiling using quantitative high-throughput screeningMenghang 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... - Profiling environmental chemicals for activity in the antioxidant response element signaling pathway using a high throughput screening approachSunita 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... 
Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitorsWenwei 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...- Identification of clinically used drugs that activate pregnane X receptorsSunita 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.... - Chemical genomics profiling of environmental chemical modulation of human nuclear receptorsRuili 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.... - Phosphodiesterase 4 inhibitors enhance sexual pleasure-seeking activity in rodentsPeixiong 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... - Identification of known drugs that act as inhibitors of NF-kappaB signaling and their mechanism of actionSusanne 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... - The pilot phase of the NIH Chemical Genomics CenterCraig 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.... - Identification of a potent new chemotype for the selective inhibition of PDE4Amanda 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... - High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell deathJennifer 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... - Paradigm shift in toxicity testing and modelingHongmao 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... - The future of toxicity testing: a focus on in vitro methods using a quantitative high-throughput screening platformSunita 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... - Predictive models for cytochrome p450 isozymes based on quantitative high throughput screening dataHongmao 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... 
High-throughput screening assays for the identification of chemical probesJames 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...- Two High Throughput Screen Assays for Measurement of TNF-α in THP-1 CellsKristin 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...