2. Academic Validation
  3. The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin

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

  • Bioorg Med Chem Lett. 2014 Jan 1;24(1):177-80. doi: 10.1016/j.bmcl.2013.11.046.
Tenna Juul Schrøder 1,  Søren Christensen 1,  Samsa Lindberg 1,  Morten Langgård 1,  Laurent David 1,  Philip J Maltas 1,  Jørgen Eskildsen 1,  Jan Jacobsen 1,  Lena Tagmose 1,  Klaus Bæk Simonsen 1,  Lars Christian Biilmann Rønn 1,  Inge E M de Jong 1,  Ibrahim J Malik 1,  Jens-Jakob Karlsson 1,  Christoffer Bundgaard 1,  Jan Egebjerg 1,  Jeffrey B Stavenhagen 1,  Dorthe Strandbygård 2,  Søren Thirup 2,  Jacob Lauwring Andersen 2,  Srinivas Uppalanchi 3,  Sridhar Pervaram 3,  Shiva Prasad Kasturi 3,  Pradheep Eradi 3,  Durga Rao Sakumudi 3,  Stephen P Watson 4
Affiliations

Affiliations

  • 1 Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark.
  • 2 The Lundbeck Foundation Research Centre MIND, Department of Molecular Biology and Genetics, Aarhus University, Gustav Wieds Vej 10C, Aarhus C 8000, Denmark.
  • 3 Medicinal Chemistry, GVK BioScience, Hyderabad, India.
  • 4 Neuroscience Drug Discovery, H. Lundbeck A/S, Copenhagen, Denmark. Electronic address: [email protected].
PMID: 24355129 DOI: 10.1016/j.bmcl.2013.11.046
Abstract

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.

Keywords

AF38469; AF40431; Neurotensin; Protein-inhibitor complex; Sortilin; Sortilin crystal structure; Sorting receptor; VPS10P.

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