{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Kumar S"],"funding":["NIGMS NIH HHS"],"pagination":["369-78"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC4384466"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["22(3)"],"pubmed_abstract":["Islet amyloid polypeptide (IAPP) is a hormone cosecreted with insulin. IAPP proceeds through a series of conformational changes from random coil to β-sheet via transient α-helical intermediates. An unknown subset of these events are associated with seemingly disparate gains of function, including catalysis of self-assembly, membrane penetration, loss of membrane integrity, mitochondrial localization, and finally, cytotoxicity, a central component of diabetic pathology. A series of small molecule, α-helical mimetics, oligopyridylamides, was previously shown to target the membrane-bound α-helical oligomeric intermediates of IAPP. In this study, we develop an improved, microwave-assisted synthesis of oligopyridylamides. A series of designed tripyridylamides demonstrate that lipid-catalyzed se"],"journal":["Chemistry & biology"],"pubmed_title":["Islet amyloid-induced cell death and bilayer integrity loss share a molecular origin targetable with oligopyridylamide-based α-helical mimetics."],"pmcid":["PMC4384466"],"funding_grant_id":["T32 GM008283","R01 GM094693","T32 GM007223","GM094693"],"pubmed_authors":["Schlamadinger DE","Hamilton AD","Miranker AD","Brown MA","Saraogi I","Hebda JA","Dunn JM","Mercado B","Kumar S","Rhoades E"],"additional_accession":[]},"is_claimable":false,"name":"Islet amyloid-induced cell death and bilayer integrity loss share a molecular origin targetable with oligopyridylamide-based α-helical mimetics.","description":"Islet amyloid polypeptide (IAPP) is a hormone cosecreted with insulin. IAPP proceeds through a series of conformational changes from random coil to β-sheet via transient α-helical intermediates. An unknown subset of these events are associated with seemingly disparate gains of function, including catalysis of self-assembly, membrane penetration, loss of membrane integrity, mitochondrial localization, and finally, cytotoxicity, a central component of diabetic pathology. A series of small molecule, α-helical mimetics, oligopyridylamides, was previously shown to target the membrane-bound α-helical oligomeric intermediates of IAPP. In this study, we develop an improved, microwave-assisted synthesis of oligopyridylamides. A series of designed tripyridylamides demonstrate that lipid-catalyzed se","dates":{"release":"2015-01-01T00:00:00Z","publication":"2015 Mar","modification":"2025-04-22T10:27:23.664Z","creation":"2019-03-27T01:49:20Z"},"accession":"S-EPMC4384466","cross_references":{"pubmed":["25754474"],"doi":["10.1016/j.chembiol.2015.01.006"]}}