Show simple item record

dc.contributor.authorCzarna, Anna Lucja
dc.contributor.authorJinhua, Wang
dc.contributor.authorZelencova, Diana
dc.contributor.authorLiu, Yao
dc.contributor.authorDeng, Xianming
dc.contributor.authorChoi, Hwan Geun
dc.contributor.authorZhang, Tinghu
dc.contributor.authorZhou, Wenjun
dc.contributor.authorChang, Jae Won
dc.contributor.authorKildalsen, Hanne
dc.contributor.authorSeternes, Ole Morten
dc.contributor.authorGray, Nathanael S.
dc.contributor.authorEngh, Richard Alan
dc.contributor.authorRothweiler, Ulli
dc.date.accessioned2019-03-14T13:54:52Z
dc.date.available2019-03-14T13:54:52Z
dc.date.issued2018-08-10
dc.description.abstractDYRK1A is one of five members of the dual-specificity tyrosine (Y) phosphorylation-regulated kinase (DYRK) family. The DYRK1A gene is located in the Down syndrome critical region and regulates cellular processes related to proliferation and differentiation of neuronal progenitor cells during early development. This has focused research on its role in neuronal degenerative diseases, including Alzheimer’s and Down syndrome. Recent studies have also shown a possible role of DYRK1A in diabetes. Here we report a variety of scaffolds not generally known for DYRK1A inhibition, demonstrating their effects in in vitro assays and also in cell cultures. These inhibitors effectively block the tau phosphorylation that is a hallmark of Alzheimer’s disease. The crystal structures of these inhibitors support the design of optimized and novel therapeutics.en_US
dc.description.sponsorshipNorthern Norway Regional Health Authorityen_US
dc.descriptionAccepted manuscript version. Published version available at <a href=https://doi.org/10.1021/acs.jmedchem.7b01847>https://doi.org/10.1021/acs.jmedchem.7b01847. </a>en_US
dc.identifier.citationCzarna, A.L., Wang, J., Zelencova, D., Liu, Y., Deng, X., Choi, H.G. ... Rothweiler, U. (2018). Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors. <i>Journal of Medicinal Chemistry, 61</i>(17), 7560-7572. https://doi.org/10.1021/acs.jmedchem.7b01847en_US
dc.identifier.cristinIDFRIDAID 1618183
dc.identifier.doi10.1021/acs.jmedchem.7b01847
dc.identifier.issn0022-2623
dc.identifier.issn1520-4804
dc.identifier.urihttps://hdl.handle.net/10037/14980
dc.language.isoengen_US
dc.publisherAmerican Chemical Societyen_US
dc.relation.journalJournal of Medicinal Chemistry
dc.relation.projectIDinfo:eu-repo/grantAgreement/RCN/SYNKNØYT/ 247732/Norway/Reisestøtte, synkrotron- og nøytronforskning, 2015-2017//en_US
dc.rights.accessRightsopenAccessen_US
dc.subjectVDP::Medical disciplines: 700::Basic medical, dental and veterinary science disciplines: 710en_US
dc.subjectVDP::Medisinske Fag: 700::Basale medisinske, odontologiske og veterinærmedisinske fag: 710en_US
dc.subjectVDP::Mathematics and natural science: 400::Chemistry: 440en_US
dc.subjectVDP::Matematikk og Naturvitenskap: 400::Kjemi: 440en_US
dc.titleNovel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitorsen_US
dc.typeJournal articleen_US
dc.typeTidsskriftartikkelen_US
dc.typePeer revieweden_US


File(s) in this item

Thumbnail

This item appears in the following collection(s)

Show simple item record