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

Schrøder, Tenna Juul; Christensen, Søren; Lindberg, Samsa; Langgård, Morten; David, Laurent; Maltas, Philip J; Eskildsen, Jørgen; Jacobsen, Jan; Tagmose, Lena; Simonsen, Klaus Bæk; Biilmann Rønn, Lars Christian; de Jong, Inge E M; Malik, Ibrahim J; Karlsson, Jens-Jakob; Bundgaard, Christoffer; Egebjerg, Jan; Stavenhagen, Jeffrey B; Strandbygård, Dorthe; Thirup, Søren; Andersen, Jacob Lauwring; Uppalanchi, Srinivas; Pervaram, Sridhar; Kasturi, Shiva Prasad; Eradi, Pradheep; Sakumudi, Durga Rao; Watson, Stephen P.

Bioorg Med Chem Lett ; 24(1): 177-80, 2014 Jan 01.

Article in English | MEDLINE | ID: mdl-24355129

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.

Subject(s)

Adaptor Proteins, Vesicular Transport/antagonists & inhibitors , Hydrocarbons, Fluorinated/pharmacology , Pyridines/pharmacology , Administration, Oral , Animals , Biological Availability , Crystallography, X-Ray , Dose-Response Relationship, Drug , High-Throughput Screening Assays , Hydrocarbons, Fluorinated/chemical synthesis , Hydrocarbons, Fluorinated/chemistry , Models, Molecular , Molecular Structure , Pyridines/chemical synthesis , Pyridines/chemistry , Rats , Structure-Activity Relationship

ABSTRACT

Subject(s)

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