On the way to precision formulation additives: 2D-screening to select solubilizers with tailored host and release capabilities

Autor: Michael G. Weller, Hans G. Börner, Claudia Donth, Dario Remmler, Timm Schwaar, Eva Maria Mandelkow, Marcus Pickhardt

Publikováno v: Journal of controlled release 285, 96-105 (2018). doi:10.1016/j.jconrel.2018.06.032

A 2-dimensional high-throughput screening method is presented to select peptide sequences from large peptide libraries for precision formulation additives, having a high capacity to specifically host a drug of interest and provide tailored drug relea

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f1ac93519bbebd49fe45f93cacb76a8d
https://doi.org/10.1016/j.jconrel.2018.06.032

Screening of a neuronal cell model of tau pathology for therapeutic compounds

Autor: Ana Kitanovic, Philip Denner, Birgit Kurkowsky, Eckhard Mandelkow, Marcus Pickhardt, Michele Tassoni, Eugenio Fava, Christoph Möhl

Publikováno v: Neurobiology of aging 76, 24-34 (2019). doi:10.1016/j.neurobiolaging.2018.11.026
Neurobiology of Aging

We have developed a cell-based phenotypic automated high-content screening approach for N2a cells expressing the pro-aggregant repeat domain of tau protein (tauRDΔK), which allows analysis of a chemogenomic library of 1649 compounds for their effect

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63359b71f283a4cc942fb1b106c4cee1

Structural Basis of Small Molecule Targetability of Monomeric Tau Protein

Autor: Attila Keresztes, Georgina Csizmadia, Róbert Gábor Kiss, Max Zhu, Eckhard Mandelkow, Gergely Tóth, Marcus Pickhardt, Katalin Solti

Publikováno v: ACS chemical neuroscience 9(12), 2997-3006 (2018). doi:10.1021/acschemneuro.8b00182

The therapeutic targeting of intrinsically disordered proteins (IDPs) by small molecules has been a challenge due to their heterogeneous conformational ensembles. A potential therapeutic strategy to alleviate the aggregation of IDPs is to maintain th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd92d165efcc160fe586b37376af2f18
https://pubmed.ncbi.nlm.nih.gov/29944336

Selection and Characterization of Tau Binding ᴅ-Enantiomeric Peptides with Potential for Therapy of Alzheimer Disease

Autor: Eckhard Mandelkow, Judith Schuster, Deniz Yolcu, Marwa Nidal Malhis, Heinrich Sticht, Susanne Aileen Funke, Anselm H. C. Horn, Marcus Pickhardt, Nadja Will, Dieter Willbold, Laura Kukuk, Christina Dammers

Publikováno v: PLoS ONE
PLoS one 11(12), e0167432 (2016). doi:10.1371/journal.pone.0167432
PLOS ONE 11(12), e0167432 (2016). doi:10.1371/journal.pone.0167432
PLoS ONE, Vol 11, Iss 12, p e0167432 (2016)

A variety of neurodegenerative disorders, including Alzheimer disease (AD), are associated with neurofibrillary tangles composed of the tau protein, as well as toxic tau oligomers. Inhibitors of pathological tau aggregation, interrupting tau self-ass

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba7e2bfaee26bf6d7ab1284c89e692cb
http://europepmc.org/articles/PMC5179029

Inhibition of Tau Filament Formation by Conformational Modulation

Autor: Markus Zweckstetter, Michal J. Gajda, Christian Griesinger, Pornsuwan Soraya, Eckhard Mandelkow, Elias Akoury, Marcus Pickhardt, Jacek Biernat

Publikováno v: Journal of the American Chemical Society 135(7), 2853-2862 (2013). doi:10.1021/ja312471h
Journal of the American Chemical Society
Journal of the American Chemical Society 135, 2853-2862 (2013). doi:10.1021/ja312471h

Antiaggregation drugs play an important role in therapeutic approaches for Alzheimer’s disease. Although a large number of small molecules that inhibit the aggregation of the tau protein have been identified, little is known about their mode of act

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea7c65ce2310a648050d6c5a88f46ae6
https://doi.org/10.1021/ja312471h