Literature DB >> 24355129

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

Tenna Juul Schrøder1, Søren Christensen1, Samsa Lindberg1, Morten Langgård1, Laurent David1, Philip J Maltas1, Jørgen Eskildsen1, Jan Jacobsen1, Lena Tagmose1, Klaus Bæk Simonsen1, Lars Christian Biilmann Rønn1, Inge E M de Jong1, Ibrahim J Malik1, Jens-Jakob Karlsson1, Christoffer Bundgaard1, Jan Egebjerg1, Jeffrey B Stavenhagen1, Dorthe Strandbygård2, Søren Thirup2, Jacob Lauwring Andersen2, Srinivas Uppalanchi3, Sridhar Pervaram3, Shiva Prasad Kasturi3, Pradheep Eradi3, Durga Rao Sakumudi3, Stephen P Watson4.   

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.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

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

Mesh:

Substances:

Year:  2013        PMID: 24355129     DOI: 10.1016/j.bmcl.2013.11.046

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  15 in total

1.  Revisiting the structure of the Vps10 domain of human sortilin and its interaction with neurotensin.

Authors:  Esben M Quistgaard; Morten K Grøftehauge; Peder Madsen; Lone T Pallesen; Brian Christensen; Esben S Sørensen; Poul Nissen; Claus M Petersen; Søren S Thirup
Journal:  Protein Sci       Date:  2014-07-22       Impact factor: 6.725

2.  Hepatocyte sortilin 1 knockout and treatment with a sortilin 1 inhibitor reduced plasma cholesterol in Western diet-fed mice.

Authors:  Cheng Chen; Jibiao Li; David J Matye; Yifeng Wang; Tiangang Li
Journal:  J Lipid Res       Date:  2019-01-22       Impact factor: 5.922

3.  Sortilin facilitates VLDL-B100 secretion by insulin sensitive McArdle RH7777 cells.

Authors:  Robert P Sparks; Wayne C Guida; Mark P Sowden; Jermaine L Jenkins; Matthew L Starr; Rutilio A Fratti; Charles E Sparks; Janet D Sparks
Journal:  Biochem Biophys Res Commun       Date:  2016-08-02       Impact factor: 3.575

Review 4.  Sortilin and Its Multiple Roles in Cardiovascular and Metabolic Diseases.

Authors:  Claudia Goettsch; Mads Kjolby; Elena Aikawa
Journal:  Arterioscler Thromb Vasc Biol       Date:  2017-11-30       Impact factor: 8.311

Review 5.  Sorting receptor sortilin-a culprit in cardiovascular and neurological diseases.

Authors:  Anne-Sophie Carlo; Anders Nykjaer; Thomas E Willnow
Journal:  J Mol Med (Berl)       Date:  2014-05-18       Impact factor: 4.599

6.  Low pH-induced conformational change and dimerization of sortilin triggers endocytosed ligand release.

Authors:  Nadia Leloup; Philip Lössl; Dimphna H Meijer; Martha Brennich; Albert J R Heck; Dominique M E Thies-Weesie; Bert J C Janssen
Journal:  Nat Commun       Date:  2017-11-22       Impact factor: 14.919

7.  Development of a Cell-Based Assay to Assess Binding of the proNGF Prodomain to Sortilin.

Authors:  Ibrahim Malik; Søren Christensen; Jeffrey B Stavenhagen; Gunnar P H Dietz
Journal:  Cell Mol Neurobiol       Date:  2017-10-24       Impact factor: 5.046

8.  Structural insights into SorCS2-Nerve Growth Factor complex formation.

Authors:  Nadia Leloup; Lucas M P Chataigner; Bert J C Janssen
Journal:  Nat Commun       Date:  2018-07-30       Impact factor: 14.919

9.  Secreted gelsolin desensitizes and induces apoptosis of infiltrated lymphocytes in prostate cancer.

Authors:  Chun-Chi Chen; Shiow-Her Chiou; Cheng-Lin Yang; Kuan-Chih Chow; Tze-Yi Lin; Hui-Wen Chang; Weir-Chiang You; Hisu-Wen Huang; Chien-Min Chen; Nien-Cheng Chen; Fen-Pi Chou; Ming-Chih Chou
Journal:  Oncotarget       Date:  2017-08-23

10.  Sortilin inhibition limits secretion-induced progranulin-dependent breast cancer progression and cancer stem cell expansion.

Authors:  Sara Rhost; Éamon Hughes; Hannah Harrison; Svanheidur Rafnsdottir; Hanna Jacobsson; Pernilla Gregersson; Ylva Magnusson; Paul Fitzpatrick; Daniel Andersson; Karoline Berger; Anders Ståhlberg; Göran Landberg
Journal:  Breast Cancer Res       Date:  2018-11-20       Impact factor: 6.466

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