Peptidotriazolamers Inhibit A beta(1-42) Oligomerization and Cross a Blood-Brain-Barrier Model

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dc.contributor.author Tonali, Nicolo
dc.contributor.author Hericks, Loreen
dc.contributor.author Schroeder, David C.
dc.contributor.author Kracker, Oliver
dc.contributor.author Krzemieniecki, Radoslaw
dc.contributor.author Kaffy, Julia
dc.contributor.author Le Joncour, Vadim
dc.contributor.author Laakkonen, Pirjo
dc.contributor.author Marion, Antoine
dc.contributor.author Ongeri, Sandrine
dc.contributor.author Dodero, Veronica I.
dc.contributor.author Sewald, Norbert
dc.date.accessioned 2022-02-16T12:35:01Z
dc.date.available 2022-02-16T12:35:01Z
dc.date.issued 2021-06
dc.identifier.citation Tonali , N , Hericks , L , Schroeder , D C , Kracker , O , Krzemieniecki , R , Kaffy , J , Le Joncour , V , Laakkonen , P , Marion , A , Ongeri , S , Dodero , V I & Sewald , N 2021 , ' Peptidotriazolamers Inhibit A beta(1-42) Oligomerization and Cross a Blood-Brain-Barrier Model ' , ChemPlusChem , vol. 86 , no. 6 , pp. 840-851 . https://doi.org/10.1002/cplu.202000814
dc.identifier.other PURE: 165400302
dc.identifier.other PURE UUID: 919e95d7-9a40-4b13-ba0e-dc09cd60e54c
dc.identifier.other WOS: 000647850200001
dc.identifier.other ORCID: /0000-0002-9620-095X/work/108462859
dc.identifier.other ORCID: /0000-0001-8153-8563/work/108466728
dc.identifier.uri http://hdl.handle.net/10138/340425
dc.description.abstract In peptidotriazolamers every second peptide bond is replaced by a 1H-1,2,3-triazole. Such foldamers are expected to bridge the gap in molecular weight between small-molecule drugs and protein-based drugs. Amyloid beta (A beta) aggregates play an important role in Alzheimer's disease. We studied the impact of amide bond replacements by 1,4-disubstituted 1H-1,2,3-triazoles on the inhibitory activity of the aggregation "hot spots" (KLVFF20)-L-16 and G(39)VVIA(42) in A beta(1-42). We found that peptidotriazolamers act as modulators of the A beta(1-42) oligomerization. Some peptidotriazolamers are able to interfere with the formation of toxic early A beta oligomers, depending on the position of the triazoles, which is also supported by computational studies. Preliminary in vitro results demonstrate that a highly active peptidotriazolamer is also able to cross the blood-brain-barrier. en
dc.format.extent 12
dc.language.iso eng
dc.relation.ispartof ChemPlusChem
dc.rights cc_by
dc.rights.uri info:eu-repo/semantics/openAccess
dc.subject &#945
dc.subject &#946
dc.subject oligomerization inhibitors
dc.subject amyloids
dc.subject foldamers
dc.subject peptidomimetics
dc.subject peptidotriazolamers
dc.subject PROTEIN-PROTEIN INTERACTIONS
dc.subject BETA-HAIRPIN MIMICS
dc.subject FOLDAMERS
dc.subject AGGREGATION
dc.subject MODULATE
dc.subject 3111 Biomedicine
dc.title Peptidotriazolamers Inhibit A beta(1-42) Oligomerization and Cross a Blood-Brain-Barrier Model en
dc.type Article
dc.contributor.organization CAN-PRO - Translational Cancer Medicine Program
dc.contributor.organization Research Programs Unit
dc.contributor.organization University of Helsinki
dc.contributor.organization Pirjo Maarit Laakkonen / Principal Investigator
dc.description.reviewstatus Peer reviewed
dc.relation.doi https://doi.org/10.1002/cplu.202000814
dc.relation.issn 2192-6506
dc.rights.accesslevel openAccess
dc.type.version publishedVersion

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