Juan J Marugan

Summary

Affiliation: National Institutes of Health
Country: USA

Publications

  1. pmc Evaluation of 2-thioxo-2,3,5,6,7,8-hexahydropyrimido[4,5-d]pyrimidin-4(1H)-one analogues as GAA activators
    Juan 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
  2. pmc Evaluation of quinazoline analogues as glucocerebrosidase inhibitors with chaperone activity
    Juan 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
  3. pmc Discovery of a novel noniminosugar acid α glucosidase chaperone series
    Jingbo 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
  4. doi request reprint Identification of small-molecule agonists of human relaxin family receptor 1 (RXFP1) by using a homogenous cell-based cAMP assay
    Catherine Z Chen
    National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, MD, USA
    J Biomol Screen 18:670-7. 2013
  5. pmc Discovery, structure-activity relationship, and biological evaluation of noninhibitory small molecule chaperones of glucocerebrosidase
    Samarjit 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
  6. pmc A high throughput glucocerebrosidase assay using the natural substrate glucosylceramide
    Omid 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
  7. doi request reprint Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor
    Samarjit Patnaik
    National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States
    J Med Chem 56:9045-56. 2013
  8. pmc A homogenous luminescence assay reveals novel inhibitors for giardia lamblia carbamate kinase
    Catherine Z Chen
    National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, USA
    Curr Chem Genomics 6:93-102. 2012
  9. pmc A high throughput screening assay system for the identification of small molecule inhibitors of gsp
    Nisan Bhattacharyya
    Skeletal Clinical Studies Unit, Craniofacial and Skeletal Diseases Branch, National Institute of Dental and Craniofacial Research, National Institutes of Health, Bethesda, Maryland, United States of America
    PLoS ONE 9:e90766. 2014
  10. pmc Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor
    R Benjamin Free
    Molecular Neuropharmacology Section, National Institute of Neurologic Disorders and Stroke, National Institutes of Health, Bethesda, Maryland R B F, L S C, A E M, B N M, T B D, J L C, A P, J A M, D R S National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland J X, X H, A E D, S T, M B G, E B, M F, N T S, J J M Cellular, Molecular, Developmental Biology and Biophysics Program, Johns Hopkins University, Baltimore, Maryland L S C Center for Molecular Recognition and Departments of Psychiatry and Pharmacology, Columbia University College of Physicians and Surgeons, and Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, New York Y H, L D, J A J Schrödinger Inc, New York, New York T B and Department of Physiology and Biophysics and Institute for Computational Biomedicine
    Mol Pharmacol 86:96-105. 2014

Collaborators

Detail Information

Publications22

  1. pmc Evaluation of 2-thioxo-2,3,5,6,7,8-hexahydropyrimido[4,5-d]pyrimidin-4(1H)-one analogues as GAA activators
    Juan 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...
  2. pmc Evaluation of quinazoline analogues as glucocerebrosidase inhibitors with chaperone activity
    Juan 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
    ....
  3. pmc Discovery of a novel noniminosugar acid α glucosidase chaperone series
    Jingbo 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...
  4. doi request reprint Identification of small-molecule agonists of human relaxin family receptor 1 (RXFP1) by using a homogenous cell-based cAMP assay
    Catherine Z Chen
    National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, MD, USA
    J Biomol Screen 18:670-7. 2013
    ..These small-molecule agonists also demonstrated selectivity against the RXFP2 receptor, providing a basis for future medicinal chemistry optimization of selective relaxin receptor agonists. ..
  5. pmc Discovery, structure-activity relationship, and biological evaluation of noninhibitory small molecule chaperones of glucocerebrosidase
    Samarjit 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...
  6. pmc A high throughput glucocerebrosidase assay using the natural substrate glucosylceramide
    Omid 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...
  7. doi request reprint Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor
    Samarjit Patnaik
    National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States
    J Med Chem 56:9045-56. 2013
    ..The pharmacokinetics and in vivo efficacy of a potent analogue in a food intake rodent model are also included, underscoring its potential therapeutic value for the treatment of sleep, anxiety, and addiction disorders. ..
  8. pmc A homogenous luminescence assay reveals novel inhibitors for giardia lamblia carbamate kinase
    Catherine Z Chen
    National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, USA
    Curr Chem Genomics 6:93-102. 2012
    ..8 with a hit rate of 0.9 % of inhibitors of glCK. Therefore, this Giardia lamblia carbamate kinase assay is useful for high throughput screening of large compound collection for identification of the inhibitors for drug development...
  9. pmc A high throughput screening assay system for the identification of small molecule inhibitors of gsp
    Nisan Bhattacharyya
    Skeletal Clinical Studies Unit, Craniofacial and Skeletal Diseases Branch, National Institute of Dental and Craniofacial Research, National Institutes of Health, Bethesda, Maryland, United States of America
    PLoS ONE 9:e90766. 2014
    ..Seven chemotypes of the major clusters were identified for further testing and analyses. ..
  10. pmc Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor
    R Benjamin Free
    Molecular Neuropharmacology Section, National Institute of Neurologic Disorders and Stroke, National Institutes of Health, Bethesda, Maryland R B F, L S C, A E M, B N M, T B D, J L C, A P, J A M, D R S National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, Maryland J X, X H, A E D, S T, M B G, E B, M F, N T S, J J M Cellular, Molecular, Developmental Biology and Biophysics Program, Johns Hopkins University, Baltimore, Maryland L S C Center for Molecular Recognition and Departments of Psychiatry and Pharmacology, Columbia University College of Physicians and Surgeons, and Division of Molecular Therapeutics, New York State Psychiatric Institute, New York, New York Y H, L D, J A J Schrödinger Inc, New York, New York T B and Department of Physiology and Biophysics and Institute for Computational Biomedicine
    Mol Pharmacol 86:96-105. 2014
    ..In summary, we have identified and characterized a novel G protein-biased agonist of the D2 dopamine receptor and identified structural features that may contribute to its biased signaling properties. ..
  11. doi request reprint Identification and optimization of small-molecule agonists of the human relaxin hormone receptor RXFP1
    Jingbo Xiao
    NIH Chemical Genomics Center, Discovery Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, USA
    Nat Commun 4:1953. 2013
    ....
  12. pmc δ-Tocopherol reduces lipid accumulation in Niemann-Pick type C1 and Wolman cholesterol storage disorders
    Miao Xu
    National Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, Maryland 20892, USA
    J Biol Chem 287:39349-60. 2012
    ..Our data suggest that regulated exocytosis may represent a potential therapeutic target for reduction of lysosomal storage in this class of diseases...
  13. pmc Discovery, synthesis, and biological evaluation of novel SMN protein modulators
    Jingbo 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...
  14. pmc 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...
  15. doi request reprint A high-throughput sphingomyelinase assay using natural substrate
    Miao 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...
  16. pmc Two high-throughput screening assays for aberrant RNA-protein interactions in myotonic dystrophy type 1
    Catherine 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...
  17. pmc High-throughput Giardia lamblia viability assay using bioluminescent ATP content measurements
    Catherine 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...
  18. 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
    ....
  19. pmc Plasma and tissue concentrations of α-tocopherol and δ-tocopherol following high dose dietary supplementation in mice
    Laura 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...
  20. pmc Novel patient cell-based HTS assay for identification of small molecules for a lysosomal storage disease
    Haifeng Geng
    McKusick Nathans Institute of Genetic Medicine, Johns Hopkins University School of Medicine, Baltimore, Maryland, USA
    PLoS ONE 6:e29504. 2011
    ....
  21. pmc Multi-gram scale synthesis of FR180204
    Samarjit 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...
  22. ncbi request reprint Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists
    Jingbo Xiao
    Discovery Innovation, NIH Chemical Genomics Center, National Center for Advancing Translational Sciences, National Institutes of Health, 9800 Medical Center Drive, Rockville, Maryland 20850, United States
    J Med Chem 57:3450-63. 2014
    ....