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

Show simple item record Tonali, Nicolo Hericks, Loreen Schroeder, David C. Kracker, Oliver Krzemieniecki, Radoslaw Kaffy, Julia Le Joncour, Vadim Laakkonen, Pirjo Marion, Antoine Ongeri, Sandrine Dodero, Veronica I. Sewald, Norbert 2022-02-16T12:35:01Z 2022-02-16T12:35:01Z 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 .
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.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 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.issn 2192-6506
dc.rights.accesslevel openAccess
dc.type.version publishedVersion

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