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

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• 作者：Tenna Juul Schr酶der ; S酶ren Christensen ; Samsa Lindberg ; Morten Langg氓rd ; Laurent David ; Philip J. Maltas ; J酶rgen Eskildsen ; Jan Jacobsen ; Lena Tagmose ; Klaus B忙k Simonsen ; Lars Christian Biilmann R酶nn ; Inge E.M. de Jong ; Ibrahim J. Malik ; Jens-Jakob Karlsson ; Christoffer Bundgaard ; Jan Egebjerg ; Jeffrey B. Stavenhagen ; Dorthe Str ; byg氓rd ; S酶ren Thirup ; Jacob Lauwring Andersen ; Srinivas Uppalanchi ; et al.
• 关键词：Sortilin ; Neurotensin ; AF38469 ; AF40431 ; VPS10P ; Sorting receptor ; Sortilin crystal structure ; Protein-inhibitor complex
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1 January, 2014
• 年：2014
• 卷：24
• 期：1
• 页码：177-180
• 全文大小：2093 K

文摘

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.