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| 001 | 888244 | ||
| 005 | 20210304134018.0 | ||
| 024 | 7 | _ | |a 10.1039/D0CB00086H |2 doi |
| 024 | 7 | _ | |a 2128/26804 |2 Handle |
| 024 | 7 | _ | |a altmetric:88804858 |2 altmetric |
| 024 | 7 | _ | |a WOS:000616568300007 |2 WOS |
| 037 | _ | _ | |a FZJ-2020-04793 |
| 082 | _ | _ | |a 540 |
| 100 | 1 | _ | |a Maity, Debabrata |0 0000-0002-4301-3106 |b 0 |e Corresponding author |
| 245 | _ | _ | |a Sub-stoichiometric inhibition of IAPP aggregation: a peptidomimetic approach to anti-amyloid agents |
| 260 | _ | _ | |a Cambridge |c 2020 |b The Royal Society of Chemistry |
| 336 | 7 | _ | |a article |2 DRIVER |
| 336 | 7 | _ | |a Output Types/Journal article |2 DataCite |
| 336 | 7 | _ | |a Journal Article |b journal |m journal |0 PUB:(DE-HGF)16 |s 1610982188_12015 |2 PUB:(DE-HGF) |
| 336 | 7 | _ | |a ARTICLE |2 BibTeX |
| 336 | 7 | _ | |a JOURNAL_ARTICLE |2 ORCID |
| 336 | 7 | _ | |a Journal Article |0 0 |2 EndNote |
| 520 | _ | _ | |a Membrane-catalysed misfolding of islet amyloid polypeptide is associated with the death of β-cells in type II diabetes (T2D). Most active compounds so far reported require high doses for inhibition of membrane bound IAPP fibrillation. Here, we describe a naphthalimide-appended oligopyridylamide-based α-helical mimetic, DM 1, for targeting membrane bound IAPP. DM 1 completely inhibits the aggregation of IAPP at doses of 0.2 equivalents. DM 1 is also effective at similarly low doses for inhibition of seed-catalyzed secondary nucleation. An NMR based study demonstrates that DM 1 modulates IAPP self-assembly by stabilizing and/or perturbing the N-terminus helix conformation. DM 1 at substoichiometric doses rescues rat insulinoma cells from IAPP-mediated cytotoxicity. Most importantly, 0.2 equivalents of DM 1 disaggregate preformed oligomers and fibrils and can reverse cytotoxicity by modulating toxic preformed oligomers and fibrils of IAPP into non-toxic conformations. |
| 536 | _ | _ | |a 553 - Physical Basis of Diseases (POF3-553) |0 G:(DE-HGF)POF3-553 |c POF3-553 |f POF III |x 0 |
| 588 | _ | _ | |a Dataset connected to CrossRef |
| 700 | 1 | _ | |a Kumar, Sunil |0 0000-0001-5472-4619 |b 1 |
| 700 | 1 | _ | |a AlHussein, Ruyof |0 P:(DE-HGF)0 |b 2 |
| 700 | 1 | _ | |a Gremer, Lothar |0 P:(DE-Juel1)145165 |b 3 |
| 700 | 1 | _ | |a Howarth, Madeline |0 P:(DE-HGF)0 |b 4 |
| 700 | 1 | _ | |a Karpauskaite, Laura |0 P:(DE-HGF)0 |b 5 |
| 700 | 1 | _ | |a Hoyer, Wolfgang |0 P:(DE-Juel1)166306 |b 6 |
| 700 | 1 | _ | |a Magzoub, Mazin |0 P:(DE-HGF)0 |b 7 |
| 700 | 1 | _ | |a Hamilton, Andrew D. |0 0000-0002-0538-175X |b 8 |e Corresponding author |
| 773 | _ | _ | |a 10.1039/D0CB00086H |0 PERI:(DE-600)3037398-0 |n 4 |p 225-232 |t RSC chemical biology |v 1 |y 2020 |x 2633-0679 |
| 856 | 4 | _ | |u https://juser.fz-juelich.de/record/888244/files/Sub-stoichiometric%20inhibition%20of%20IAPP%20aggregation%3A%20a%20peptidomimetic%20approach%20to%20anti-amyloid%20agents.pdf |y OpenAccess |
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| 910 | 1 | _ | |a Forschungszentrum Jülich |0 I:(DE-588b)5008462-8 |k FZJ |b 3 |6 P:(DE-Juel1)145165 |
| 910 | 1 | _ | |a Forschungszentrum Jülich |0 I:(DE-588b)5008462-8 |k FZJ |b 6 |6 P:(DE-Juel1)166306 |
| 913 | 1 | _ | |a DE-HGF |b Key Technologies |l BioSoft – Fundamentals for future Technologies in the fields of Soft Matter and Life Sciences |1 G:(DE-HGF)POF3-550 |0 G:(DE-HGF)POF3-553 |3 G:(DE-HGF)POF3 |2 G:(DE-HGF)POF3-500 |4 G:(DE-HGF)POF |v Physical Basis of Diseases |x 0 |
| 914 | 1 | _ | |y 2020 |
| 915 | _ | _ | |a OpenAccess |0 StatID:(DE-HGF)0510 |2 StatID |
| 915 | _ | _ | |a Creative Commons Attribution-NonCommercial CC BY-NC 3.0 |0 LIC:(DE-HGF)CCBYNC3 |2 HGFVOC |
| 920 | _ | _ | |l yes |
| 920 | 1 | _ | |0 I:(DE-Juel1)IBI-7-20200312 |k IBI-7 |l Strukturbiochemie |x 0 |
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| 980 | _ | _ | |a UNRESTRICTED |
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| 980 | 1 | _ | |a FullTexts |
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