Research Topics
| Juan J MaruganSummaryAffiliation: National Institutes of Health Country: USA Publications
| Collaborators
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Detail Information
Publications
Evaluation of 2-thioxo-2,3,5,6,7,8-hexahydropyrimido[4,5-d]pyrimidin-4(1H)-one analogues as GAA activatorsJuan J Marugan
NIH Chemical Genomic Center, National Human Genome Research Institute, National Institutes of Heath, 9800 Medical Center Drive, Rockville, MD, USA
Eur J Med Chem 45:1880-97. 2010..Herein we report our initial findings of a new series of acid alpha-glucosidase activators...- Evaluation of quinazoline analogues as glucocerebrosidase inhibitors with chaperone activityJuan J Marugan
NIH Chemical Genomic Center, National Human Genome Research Institute, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, United States
J Med Chem 54:1033-58. 2011.... - Discovery of a novel noniminosugar acid α glucosidase chaperone seriesJingbo Xiao
NIH Chemical Genomics Center, NIH Center for Translational Therapeutics, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, USA
J Med Chem 55:7546-59. 2012..AMDE and physical properties studies indicate that this series is a promising lead for further pharmacokinetic evaluation and testing in Pompe disease models... - Discovery, structure-activity relationship, and biological evaluation of noninhibitory small molecule chaperones of glucocerebrosidaseSamarjit Patnaik
NIH Chemical Genomic Center, National Center for Advancing Translation Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland, United States
J Med Chem 55:5734-48. 2012..These compounds provide the basis for the development of a novel approach toward small molecule treatment for patients with Gaucher disease... - A high throughput glucocerebrosidase assay using the natural substrate glucosylceramideOmid Motabar
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892 3370, USA
Anal Bioanal Chem 402:731-9. 2012..The assay sensitivity and robustness is similar to those seen with other glucocerebrosidase fluorescence assays. Therefore, this new glucocerebrosidase assay is an alternative approach for high throughput screening... - Discovery, synthesis, and biological evaluation of novel SMN protein modulatorsJingbo Xiao
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Rockville, Maryland 20850, USA
J Med Chem 54:6215-33. 2011..We anticipate that a lead candidate chosen from this series may serve as a useful probe for exploring the therapeutic benefits of SMN protein up-regulation in SMA animal models and a starting point for clinical development... - Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk)Bryan T Mott
NIH Chemical Genomics Center, National Human Genome Research Institute, Bethesda, MD 20892 3370, USA
Bioorg Med Chem Lett 19:6700-5. 2009..Molecular docking provides further evidence that inhibition is the result of binding at the kinase hinge region. Selected compounds represent novel tools capable of potent and selective inhibition of Clk1, Clk4, and Dyrk1A... 
A high-throughput sphingomyelinase assay using natural substrateMiao Xu
National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892 3370, USA
Anal Bioanal Chem 404:407-14. 2012..The results demonstrate the robustness and effectiveness of the natural substrate sphingomyelinase assay for screening sphingomyelinase inhibitors...- Two high-throughput screening assays for aberrant RNA-protein interactions in myotonic dystrophy type 1Catherine Z Chen
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
Anal Bioanal Chem 402:1889-98. 2012..These assays are homogenous and successfully miniaturized to 1,536-well plate format. Both assays were validated and show robust signal-to-basal ratios and Z' factors... - High-throughput Giardia lamblia viability assay using bioluminescent ATP content measurementsCatherine Z Chen
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland 20892 3370, USA
Antimicrob Agents Chemother 55:667-75. 2011..The most potent novel compound was fumagillin, which showed 50% inhibitory concentrations of 10 nM against the WB isolate and 2 nM against the GS isolate... - 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.... - Plasma and tissue concentrations of α-tocopherol and δ-tocopherol following high dose dietary supplementation in miceLaura L Baxter
Genetic Disease Research Branch, National Human Genome Research Institute, National Institutes of Health, Bethesda, MD 20892, USA
Nutrients 4:467-90. 2012..These results provide valuable PK information on high dosage α-toc and δ-toc in mouse and show that supplementation of sesamin with δ-toc further increases δ-toc levels over those seen with δ-toc supplementation alone... - Novel patient cell-based HTS assay for identification of small molecules for a lysosomal storage diseaseHaifeng Geng
McKusick Nathans Institute of Genetic Medicine, Johns Hopkins University School of Medicine, Baltimore, Maryland, USA
PLoS ONE 6:e29504. 2011.... - Multi-gram scale synthesis of FR180204Samarjit Patnaik
National Institutes of Health Chemical Genomics Center, 9800 Medical Center Drive, Rockville, Maryland 20850, USA
J Org Chem 74:8870-3. 2009..A concise synthesis of the ERK inhibitor FR180204 has been developed. The synthesis consists of six operationally simple steps and can be utilized to make multi-gram quantities of FR180204...