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The identification of AF38469: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin: An orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin

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  • Tenna Juul Schrøder, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
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  • Søren Christensen, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark., Denmark
  • Samsa Lindberg, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
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  • Morten Langgård, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
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  • Laurent David, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
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  • Philip J Maltas, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
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  • Jørgen Eskildsen, Risø National Laboratory for Sustainable Energy, Denmark
  • Jan Jacobsen, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark., Denmark
  • Lena Tagmose, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
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  • Klaus Bæk Simonsen, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
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  • Lars Christian Biilmann Rønn, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
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  • Inge Elisabeth Maria de Jong, 2012 Institut for Farmakologi og Farmakoterapi, Denmark
  • Ibrahim J Malik, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
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  • Jens-Jakob Karlsson, Department of Chemistry, Denmark
  • Christoffer Bundgaard, 2012 Institut for Farmakologi og Farmakoterapi, Denmark
  • Jan Egebjerg, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
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  • Jeffrey B Stavenhagen, Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
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  • Dorthe Strandbygård
  • Søren Skou Thirup
  • Jacob Lauwring Andersen, Denmark
  • Srinivas Uppalanchi, Medicinal Chemistry, GVK BioScience, Hyderabad, India.
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  • Sridhar Pervaram, Medicinal Chemistry, GVK BioScience, Hyderabad, India.
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  • Shiva Prasad Kasturi, Medicinal Chemistry, GVK BioScience, Hyderabad, India.
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  • Pradheep Eradi, Medicinal Chemistry, GVK BioScience, Hyderabad, India.
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  • Durga Rao Sakumudi, Medicinal Chemistry, GVK BioScience, Hyderabad, India.
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  • Stephen Paul Watson, 2012 Institut for Farmakologi og Farmakoterapi, Denmark
The identification of the novel, selective, orally bioavailable Sortilin inhibitor AF38469 is described. Structure-activity relationships and syntheses are reported, along with an X-ray crystal structure of the sortilin-AF38469 protein-inhibitor complex.
Original languageEnglish
JournalBioorganic & Medicinal Chemistry Letters
Volume24
Issue1
Pages (from-to)177-180
Number of pages4
ISSN0960-894X
DOIs
Publication statusPublished - 1 Jan 2014

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