ArticleActa crystallographica. Section D, Biological crystallography2014
Identification of the first small-molecule ligand of the neuronal receptor sortilin and structure determination of the receptor-ligand complex.
Article in Acta crystallographica. Section D, Biological crystallography, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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14 citing papers in PubMed, 35 citations in OpenAlex.
- Prosaposin maintains adult neural stem cells in a state associated with deep quiescence.Stem cell reports · 2024Article
- Carbonic Anhydrase Robustness for Use in Nanoscale COACS omega · 2023Article
- Multi-ancestry genome-wide gene-sleep interactions identify novel loci for blood pressure.Molecular psychiatry · 2021Article
- PAK Kinases Target Sortilin and Modulate Its Sorting.Molecular and cellular biology · 2020Article
- Anti-sortilin1 Antibody Up-Regulates ProgranulinFrontiers in neuroscience · 2020Article
- Sortilin gates neurotensin and BDNF signaling to control peripheral neuropathic pain.Science advances · 2019Article
- Regional and Cellular Mapping of Sortilin Immunoreactivity in Adult Human Brain.Frontiers in neuroanatomy · 2019Article
- Structural insights into SorCS2-Nerve Growth Factor complex formation.Nature communications · 2018Article
- Development of a Cell-Based Assay to Assess Binding of the proNGF Prodomain to Sortilin.Cellular and molecular neurobiology · 2018Article
- Sortilin and Its Multiple Roles in Cardiovascular and Metabolic Diseases.Arteriosclerosis, thrombosis, and vascular biology · 2018Review
- Low pH-induced conformational change and dimerization of sortilin triggers endocytosed ligand release.Nature communications · 2017Article
- Diacerein-mediated inhibition of IL-6/IL-6R signaling induces apoptotic effects on breast cancer.Oncogene · 2016Article
- Sortilin is associated with breast cancer aggressiveness and contributes to tumor cell adhesion and invasion.Oncotarget · 2015Article
- Revisiting the structure of the Vps10 domain of human sortilin and its interaction with neurotensin.Protein science : a publication of the Protein Society · 2014Article
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Authors and funding
23 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Sortilin is a type I membrane glycoprotein belonging to the vacuolar protein sorting 10 protein (Vps10p) family of sorting receptors and is most abundantly expressed in the central nervous system. Sortilin has emerged as a key player in the regulation of neuronal viability and has been implicated as a possible therapeutic target in a range of disorders. Here, the identification of AF40431, the first reported small-molecule ligand of sortilin, is reported. Crystals of the sortilin-AF40431 complex were obtained by co-crystallization and the structure of the complex was solved to 2.7 Å resolution. AF40431 is bound in the neurotensin-binding site of sortilin, with the leucine moiety of AF40431 mimicking the binding mode of the C-terminal leucine of neurotensin and the 4-methylumbelliferone moiety of AF40431 forming π-stacking with a phenylalanine.
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