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

Autor:	Søren Christensen, Ibrahim John Malik, Laurent David, Lena Tagmose, Samsa Lindberg, Tenna Juul Schrøder, Durga Rao Sakumudi, Søren Thirup, Klaus Baek Simonsen, Christoffer Bundgaard, Jan Egebjerg, Lars Christian Biilmann Rønn, Jeffrey B. Stavenhagen, Pradheep Eradi, Shiva Prasad Kasturi, Jan Jacobsen, Jørgen Eskildsen, Jacob Andersen, Inge E. M. de Jong, Philip James Maltas, Stephen P. Watson, Sridhar Pervaram, Dorthe Strandbygård, Morten Langgård, Srinivas Uppalanchi, Jens-Jakob Karlsson
Rok vydání:	2013
Předmět:	Models Molecular Hydrocarbons Fluorinated Pyridines Clinical Biochemistry Pharmaceutical Science Administration Oral Biological Availability Crystallography X-Ray Biochemistry chemistry.chemical_compound Structure-Activity Relationship Signaling proteins Drug Discovery Animals Receptor Molecular Biology Dose-Response Relationship Drug Molecular Structure Chemistry Organic Chemistry Sorting Bioavailability High-Throughput Screening Assays Rats Adaptor Proteins Vesicular Transport Molecular Medicine Identification (biology) Neurotensin
Zdroj:	Bioorganicmedicinal chemistry letters. 24(1)
ISSN:	1464-3405
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bedc826128f87085b5292d2d536c1fff https://pubmed.ncbi.nlm.nih.gov/24355129 Zobrazit plný text záznamu Full Text from ScienceDirect