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Research Article

High-Affinity Inhibitors of Human NAD+-Dependent 15-Hydroxyprostaglandin Dehydrogenase: Mechanisms of Inhibition and Structure-Activity Relationships

  • Frank H. Niesen,

    Affiliation: Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, United Kingdom

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  • Lena Schultz,

    Affiliation: NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, United States of America

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  • Ajit Jadhav,

    Affiliation: NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, United States of America

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  • Chitra Bhatia,

    Affiliation: Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, United Kingdom

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  • Kunde Guo,

    Affiliation: Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, United Kingdom

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  • David J. Maloney,

    Affiliation: NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, United States of America

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  • Ewa S. Pilka,

    Affiliation: Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, United Kingdom

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  • Minghua Wang,

    Affiliation: Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, United Kingdom

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  • Udo Oppermann,

    Affiliations: NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, United States of America, Biomedical Research Unit, Nuffield Department of Orthopedic Surgery, Rheumatology and Musculoskeletal Sciences, Botnar Research Center, University of Oxford, Oxford, United Kingdom

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  • Tom D. Heightman,

    Affiliation: Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, United Kingdom

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  • Anton Simeonov mail

    asimeono@mail.nih.gov

    Affiliation: NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, United States of America

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  • Published: November 02, 2010
  • DOI: 10.1371/journal.pone.0013719
  • Published in PLOS ONE

About the Authors

Frank H. Niesen, Chitra Bhatia, Kunde Guo, Ewa S. Pilka, Minghua Wang, Tom D. Heightman
Structural Genomics Consortium, Nuffield Department of Clinical Medicine, University of Oxford, Oxford, United Kingdom
Lena Schultz, Ajit Jadhav, David J. Maloney, Udo Oppermann, Anton Simeonov
NIH Chemical Genomics Center, National Human Genome Research Institute, National Institutes of Health, Bethesda, Maryland, United States of America
Udo Oppermann
Biomedical Research Unit, Nuffield Department of Orthopedic Surgery, Rheumatology and Musculoskeletal Sciences, Botnar Research Center, University of Oxford, Oxford, United Kingdom

Corresponding Author

Email: asimeono@mail.nih.gov

Competing Interests

The authors have declared that no competing interests exist.

Author Contributions

Conceived and designed the experiments: FHN DM UO TDH AS. Performed the experiments: FHN LS CB KG DM ESP. Analyzed the data: FHN LS AJ CB DM ESP MW UO TDH AS. Contributed reagents/materials/analysis tools: FHN AJ DM. Wrote the paper: FHN AJ DM UO TDH AS.