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

Autor: 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.

Publikováno v: In Bioorganic & Medicinal Chemistry Letters 1 January 2014 24(1):177-180

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

Autor: 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 Elisabeth Maria, Malik, Ibrahim J, Karlsson, Jens-Jakob, Bundgaard, Christoffer, Egebjerg, Jan, Stavenhagen, Jeffrey B, Strandbygård, Dorthe, Thirup, Søren Skou, Andersen, Jacob Lauwring, Uppalanchi, Srinivas, Pervaram, Sridhar, Kasturi, Shiva Prasad, Eradi, Pradheep, Sakumudi, Durga Rao, Watson, Stephen Paul

Publikováno v: Schrøder, T J, Christensen, S, Lindberg, S, Langgård, M, David, L, Maltas, P J, Eskildsen, J, Jacobsen, J, Tagmose, L, Simonsen, K B, Biilmann Rønn, L C, de Jong, I E M, Malik, I J, Karlsson, J-J, Bundgaard, C, Egebjerg, J, Stavenhagen, J B, Strandbygård, D, Thirup, S S, Andersen, J L, Uppalanchi, S, Pervaram, S, Kasturi, S P, Eradi, P, Sakumudi, D R & Watson, S P 2014, ' 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 ', Bioorganic & Medicinal Chemistry Letters, vol. 24, no. 1, pp. 177-180 . https://doi.org/10.1016/j.bmcl.2013.11.046

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 comp

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