Novel Sulfonanilide Inhibitors of SHIP2 Enhance Glucose Uptake into Cultured Myotubes

Show simple item record

dc.contributor.author Berg, Mika Erik Anthon
dc.contributor.author Naams, Jette-Britt
dc.contributor.author Hautala, Laura
dc.contributor.author Tolvanen, Tuomas
dc.contributor.author Ahonen, Jari
dc.contributor.author Lehtonen, Sanna
dc.contributor.author Wähälä, Kristiina
dc.date.accessioned 2020-07-16T12:26:01Z
dc.date.available 2020-07-16T12:26:01Z
dc.date.issued 2020-01-28
dc.identifier.citation Berg , M E A , Naams , J-B , Hautala , L , Tolvanen , T , Ahonen , J , Lehtonen , S & Wähälä , K 2020 , ' Novel Sulfonanilide Inhibitors of SHIP2 Enhance Glucose Uptake into Cultured Myotubes ' , ACS Omega , vol. 5 , no. 3 , pp. 1430-1438 . https://doi.org/10.1021/acsomega.9b02944
dc.identifier.other PURE: 130083812
dc.identifier.other PURE UUID: a9aaf11d-6e68-4423-8f29-e7874802ecbc
dc.identifier.other WOS: 000510000900019
dc.identifier.other ORCID: /0000-0003-4082-8622/work/77475956
dc.identifier.other ORCID: /0000-0003-4189-2415/work/77477844
dc.identifier.uri http://hdl.handle.net/10138/317780
dc.description.abstract A series of substituted sulfonanilide analogs were prepared and evaluated as novel potent inhibitors of SH2 domaincontaining inositol polyphosphate 5′-phosphatase 2 (SHIP2). SHIP2 has been shown to be a new attractive target for the treatment of insulin resistance in type 2 diabetes mellitus (T2D), which can lead to life-threatening diabetic kidney disease (DKD). Amongst the synthesized compounds, the two most promising candidates, 10 and 11, inhibited SHIP2 significantly. Additionally, these compounds induced Akt activation in a dose-dependent manner, increased the presence of glucose transporter 4 at the plasma membrane, and enhanced glucose uptake in cultured myotubes in vitro at lower concentrations than metformin, the most widely used antidiabetic drug. These results show that the novel SHIP2 inhibitors have insulin sensitizing capacity and provide prototypes for further drug development for T2D and DKD. en
dc.format.extent 9
dc.language.iso eng
dc.relation.ispartof ACS Omega
dc.rights cc_by
dc.rights.uri info:eu-repo/semantics/openAccess
dc.subject 5'-PHOSPHATASE-2 GENE POLYMORPHISMS
dc.subject ASSOCIATION
dc.subject CELLS
dc.subject INOSITOL
dc.subject INPPL1
dc.subject METFORMIN
dc.subject PHOSPHATASE
dc.subject PLASMA-MEMBRANE
dc.subject STIMULATION
dc.subject SULFONYLUREAS
dc.subject 116 Chemical sciences
dc.subject 3121 General medicine, internal medicine and other clinical medicine
dc.title Novel Sulfonanilide Inhibitors of SHIP2 Enhance Glucose Uptake into Cultured Myotubes en
dc.type Article
dc.contributor.organization Research Services
dc.contributor.organization Doctoral Programme in Chemistry and Molecular Sciences
dc.contributor.organization Department of Chemistry
dc.contributor.organization Diabetes and Obesity Research Program
dc.contributor.organization Doctoral Programme in Biomedicine
dc.contributor.organization Sanna Lehtonen research group
dc.contributor.organization Doctoral Programme in Integrative Life Science
dc.contributor.organization Department of Pathology
dc.contributor.organization Doctoral Programme in Drug Research
dc.contributor.organization Medicum
dc.description.reviewstatus Peer reviewed
dc.relation.doi https://doi.org/10.1021/acsomega.9b02944
dc.relation.issn 2470-1343
dc.rights.accesslevel openAccess
dc.type.version publishedVersion

Files in this item

Total number of downloads: Loading...

Files Size Format View
acsomega.9b02944.pdf 1.344Mb PDF View/Open

This item appears in the following Collection(s)

Show simple item record