- Kutzsche J, Guzman GA, Willuweit A, Kletke O, Wollert E, Gering I, Jürgens D, Breitkreutz J, Stark H, Beck-Sickinge AG, Klöcker N, Hidalgo P, Willbold D.
An orally available N-type calcium channel inhibitor for the treatment of neuropathic pain.
Br J Pharmacol. , (2023)
https://pubmed.ncbi.nlm.nih.gov/38157867/
- Kutzsche J, Schemmert S, Bujnicki T, Zafiu C, Halbgebauer S, Kraemer-Schulien V, Pils M, Blömeke L, Post J, Kulawik A, Jürgens D, Rossberg WM, Hümpel M, Bannach O, Otto M, Araujo JA, Willuweit A, Willbold D.
Oral treatment with the all-d-peptide RD2 enhances cognition in aged beagle dogs - A model of sporadic Alzheimer's disease
Heliyon 29;9(8):e18443, (2023)
https://pubmed.ncbi.nlm.nih.gov/37609390/
- Wintz K, Post J, Langen K-J, Willbold D, Willuweit A, Kutzsche J
Oral Treatment with d-RD2RD2 Impedes Early Disease Mechanisms in SOD1*G93A Transgenic Mice but Does Not Prolong Survival
Biomedicines 11(4), 995, (2023)
https://doi.org/10.3390/biomedicines11040995
https://www.mdpi.com/2227-9059/11/4/995
- Kass B, Schemmert S, Zafiu C, Pils M, Bannach O, Kutzsche J, Bujnicki T, Willbold D.
Aβ oligomer concentration in mouse and human brain and its drug-induced reduction ex vivo.
Cell Rep Med. 3(5):100630, (2022)
https://doi.org/10.1016/j.xcrm.2022.100630
- Sevenich M, Honold D, Willuweit A, Kutzsche J, Mohrlüder J, Willbold D.
Development of an α-synuclein fibril and oligomer specific tracer for diagnosis of Parkinson's disease, dementia with Lewy bodies and multiple system atrophy.
Neurochem Int. 161, 105422 (2022)
https://doi.org/10.1016/j.neuint.2022.105422
https://pubmed.ncbi.nlm.nih.gov/36252819/
- Bocharov, E. V., L. Gremer, A. S. Urban, I. S. Okhrimenko, P. E. Volynsky, K. D. Nadezhdin, O. V. Bocharova, D. A. Kornilov, Y. A. Zagryadskaya, A. V. Kamynina, P. K. Kuzmichev, J. Kutzsche, N. Bolakhrif, A. Müller-Schiffmann, N. A. Dencher, A. S. Arseniev, R. G. Efremov, V. I. Gordeliy and D. Willbold
All-d-Enantiomeric Peptide D3 Designed for Alzheimer’s Disease Treatment Dynamically Interacts with Membrane-Bound Amyloid-β Precursors.
Journal of Medicinal Chemistry , (2021)
https://doi.org/10.1021/acs.jmedchem.1c00632
- Camargo LC, Honold D, Bauer R, Shah NJ, Langen KJ, Willbold D, Kutzsche J, Willuweit A, Schemmert S.
Sex-Related Motor Deficits in the Tau-P301L Mouse Model
Biomedicines 9(9):1160, (2021)
https://pubmed.ncbi.nlm.nih.gov/34572348/
- Camargo LC, Schöneck M, Sangarapillai N, Honold D, Shah NJ, Langen KJ, Willbold D, Kutzsche J, Schemmert S, Willuweit A
PEAβ Triggers Cognitive Decline and Amyloid Burden in a Novel Mouse Model of Alzheimer's Disease
Int J Mol Sci. 22(13):706, (2021)
https://pubmed.ncbi.nlm.nih.gov/34209113/
- Post J, Kogel V, Schaffrath A, Lohmann P, Shah NJ, Langen K-J, Willbold D, Willuweit A, Kutzsche J
A Novel Anti-Inflammatory d-Peptide Inhibits Disease Phenotype Progression in an ALS Mouse Model.
Molecules 26(6):1590, (2021)
https://doi.org/10.3390/molecules26061590
- Post J, Schaffrath A, Gering I, Hartwig S, Lehr S, Shah NJ, Langen KJ, Willbold D, Kutzsche J, Willuweit A.
Oral Treatment with RD2RD2 Impedes Development of Motoric Phenotype and Delays Symptom Onset in SOD1 G93A Transgenic Mice
Int J Mol Sci . 22(13):7066, (2021)
https://pubmed.ncbi.nlm.nih.gov/34209129/
- Elfgen A, Santiago-Schübel B, Hupert M, Schemmert S, Schartmann E, Tusche M, Gering I, Zafiu C, Kutzsche J.
Oral absorption enhancement of the amyloid-β oligomer eliminating compound RD2 by conjugation with folic acid
Eur J Pharm Sci. , (2020)
https://pubmed.ncbi.nlm.nih.gov/33035662/
- Kutzsche J, Jürgens D, Willuweit A, Adermann K, Fuchs C, Simons S, Windisch M, Hümpel M, Rossberg W, Wolzt M, Willbold D.
Safety and Pharmacokinetics of the Orally Available Antiprionic Compound PRI-002: A Single and Multiple Ascending Dose Phase I Study
Alzheimers Dement (N Y) , 20;6(1):e12001 (2020)
https://pubmed.ncbi.nlm.nih.gov/32211506/
- Dieter Willbold and Janine Kutzsche
Do We Need Anti-Prion Compounds to Treat Alzheimer’s Disease?
Molecules 24, 2237 (2019)
https://www.mdpi.com/1420-3049/24/12/2237
- Elfgen A, Hupert M, Bochinsky K, Tusche M, González de San Román Martin E, Gering I, Sacchi S, Pollegioni L, Huesgen PF, Hartmann R, Santiago-Schübel B, Kutzsche J, Willbold D.
Metabolic resistance of the D-peptide RD2 developed for direct elimination of amyloid-β oligomers
Sci Rep 9(1), 5715 (2019)
http://10.1038/s41598-019-41993-6
https://www.nature.com/articles/s41598-019-41993-6
- Schemmert S, Schartmann E, Honold D, Zafiu C, Ziehm T, Langen KJ, Shah NJ, Kutzsche J, Willuweit A, Willbold D.
Deceleration of the neurodegenerative phenotype in pyroglutamate-Aβ accumulating transgenic mice by oral treatment with the Aβ oligomer eliminating compound RD2.
Neurobiol Dis. 124, 36-45 (2019)
https://www.sciencedirect.com/science/article/pii/S0969996118307320
- Schemmert S, Schartmann E, Zafiu C, Kass B, Hartwig S, Lehr S, Bannach O, Langen KJ, Shah NJ, Kutzsche J, Willuweit A, Willbold D.
Aβ Oligomer Elimination Restores Cognition in Transgenic Alzheimer's Mice with Full-blown Pathology.
Mol Neurobiol. 56(3):, 2211-2223 (2019)
https://10.1007/s12035-018-1209-3
https://www.ncbi.nlm.nih.gov/pubmed/30003517
- Zhang T, Gering I, Kutzsche J, Nagel-Steger L, Willbold D.
Toward the Mode of Action of the Clinical Stage All-d-Enantiomeric Peptide RD2 on Aβ42 Aggregation.
ACS Chem Neurosci. 10(12), 4800-4809. (2019)
https://pubs.acs.org/doi/10.1021/acschemneuro.9b00458
https://www.ncbi.nlm.nih.gov/pubmed/31710458
- Cavini IA, Munte CE, Erlach MB, van Groen T, Kadish I, Zhang T, Ziehm T, Nagel-Steger L, Kutzsche J, Kremer W, Willbold D, Kalbitzer HR.
Inhibition of amyloid Aβ aggregation by high pressures or specific d-enantiomeric peptides.
Chem Commun (Camb). 54(26), 3294-3297 (2018)
https://10.1039/c8cc01458b.
https://www.ncbi.nlm.nih.gov/pubmed/29537428
- Dunkelmann T, Teichmann K, Ziehm T, Schemmert S, Frenzel D, Tusche M, Dammers C, Jürgens D, Langen KJ, Demuth HU, Shah NJ, Kutzsche J, Willuweit A, Willbold D
Aβ oligomer eliminating compounds interfere successfully with pEAβ (3–42) induced motor neurodegenerative phenotype in transgenic mice
Neuropeptides 67, 27-35 (2018)
https://doi.org/10.1016/j.npep.2017.11.011
https://www.sciencedirect.com/science/article/pii/S0143417917301531
- Dunkelmann T, Schemmert S, Honold D, Teichmann K, Butzküven E, Demuth HU, Shah NJ, Langen KJ, Kutzsche J, Willbold D, Willuweit A.
Comprehensive Characterization of the Pyroglutamate Amyloid-β Induced Motor Neurodegenerative Phenotype of TBA2.1 Mice.
J Alzheimers Dis. 63(1), 115-130 (2018)
https://10.3233/JAD-170775
https://www.ncbi.nlm.nih.gov/pubmed/29578479
- Schartmann E, Schemmert S, Niemietz N, Honold D, Ziehm T, Tusche M, Elfgen A, Gering I, Brener O, Shah NJ, Langen KJ, Kutzsche J, Willbold D, Willuweit A.
In Vitro Potency and Preclinical Pharmacokinetic Comparison of All-D-Enantiomeric Peptides Developed for the Treatment of Alzheimer's Disease.
J Alzheimers Dis 64(3), 859-873 (2018)
https://10.3233/JAD-180165
https://www.ncbi.nlm.nih.gov/pubmed/29966196
- Elfgen A, Santiago-Schübel B, Gremer L, Kutzsche J, Willbold, D
Surprisingly high stability of the Aβ oligomer eliminating all-D-enantiomeric peptide D3 in media simulating the route of orally administered drugs
European Journal of Pharmaceutical Sciences 107, 203-207 (2017)
https://doi.org/10.1016/j.ejps.2017.07.015
https://www.ncbi.nlm.nih.gov/pubmed/28711713
- Hupert M, Elfgen A, Schartmann E, Schemmert S, Buscher B, Kutzsche J, Willbold D, Santiago-Schübel B
Development and Validation of an UHPLC-ESI-QTOF-MS method for quantification of the highly hydrophilic amyloid-β oligomer eliminating all-D-enantiomeric peptide RD2 in mouse plasma
Journal of Chromatography B 1073, 123-129 (2017)
https://doi.org/10.1016/j.jchromb.2017.12.009
https://www.sciencedirect.com/science/article/pii/S1570023217316562
- Klein AN, Ziehm T, van Groen T, Kadish I, Elfgen A, Tusche M, Thomaier M, Reiss K, Brener O, Gremer L, Kutzsche J, Willbold D
Optimization of D-peptides for Aβ monomer binding specificity enhances their potential to eliminate toxic Aβ oligomers
ACS Chem Neurosci 8, 1889-1900 (2017)
- Kutzsche J, Schemmert S, Tusche M, Neddens J, Rabl R, Jürgens D, Brener O, Willuweit A, Hutter-Paier B, Willbold D.
Large-Scale Oral Treatment Study with the Four Most Promising D3-Derivatives for the Treatment of Alzheimer's Disease.
Molecules 22(10), (2017)
http://10.3390/molecules22101693
https://www.ncbi.nlm.nih.gov/pubmed/28994710
- Schartmann E, Schemmert S, Ziehm T, Leithold LHE, Jiang N, Tusche M, Shah NJ, Langen KJ, Kutzsche J, Willbold D, Willuweit A.
Comparison of blood-brain barrier penetration efficiencies between linear and cyclic all-d-enantiomeric peptides developed for the treatment of Alzheimer's disease.
Eur J Pharm Sci. 17, 0928-0987 (2017)
https://doi.org/10.1016/j.ejps.2017.12.005
https://www.ncbi.nlm.nih.gov/pubmed/29225107
- van Groen T, Schemmert S, Brener O, Gremer L, Ziehm T, Tusche M, Nagel-Steger L, Kadish I, Schartmann E, Elfgen A, Jürgens D, Willuweit A, Kutzsche J, Willbold D.
The Aβ oligomer eliminating D-enantiomeric peptide RD2 improves cognition without changing plaque pathology.
Sci Rep. 7, 16275 (2017)
https://doi.org/10.1038/s41598-017-16565-1
https://www.nature.com/articles/s41598-017-16565-1
- Klein AN, Ziehm T, Tusche M, Buitenhuis J, Bartnik D, Boeddrich A, Wiglenda T, Wanker E, Funke SA, Brener O, Gremer L, Kutzsche J, Willbold D.
Optimization of the All-D Peptide D3 for Aβ Oligomer Elimination.
PLoS One 11(4), (2016)
http://dx.doi.org/10.1371/journal.pone.0153035
Erratum in: PLoS One. 2016;11(7):e0158960. http://dx.doi.org/10.1371/journal.pone.0158960
- Leithold LH, Jiang N, Post J, Niemietz N, Schartmann E, Ziehm T, Kutzsche J, Shah NJ, Breitkreutz J, Langen KJ, Willuweit A, Willbold D.
Pharmacokinetic properties of tandem D-peptides designed for treatment of Alzheimer's disease
Eur. J. Pharm. Sci. 89, 31-38 (2016)
http://dx.doi.org/10.1016/j.ejps.2016.04.016
- Leithold LH, Jiang N, Post J, Ziehm T, Schartmann E, Kutzsche J, Shah NJ, Breitkreutz J, Langen KJ, Willuweit A, Willbold D.
Pharmacokinetic Properties of a Novel D-Peptide Developed to be Therapeutically Active Against Toxic β-Amyloid Oligomers
Pharm Res. 33, 328-336 (2016)
- Rudolph S, Klein AN, Tusche M, Schlosser C, Elfgen A, Brener O, Teunissen C,Gremer L, Funke SA, Kutzsche J, Willbold D.
Correction: Competitive Mirror Image Phage Display Derived Peptide Modulates Amyloid Beta Aggregation and Toxicity
PLoS One 11(7), (2016)
http://dx.doi.org/10.1371/journal.pone.0159470
http://journals.plos.org/plosone/article?id=info:doi/10.1371/journal.pone.0159470
- Rudolph S, Klein AN, Tusche M, Schlosser C, Elfgen A, Brener O, Teunissen C, Gremer L, Funke SA, Kutzsche J, Willbold D.
Competitive Mirror Image Phage Display Derived Peptide Modulates Amyloid Beta Aggregation and Toxicity.
PLoS One 11(2):e0147470., (2016)
http://dx.doi.org/10.1371/journal.pone.0147470
http://journals.plos.org/plosone/article?id=10.1371/journal.pone.0147470
- Ziehm T, Brener O, van Groen T, Kadish I, Frenzel D, Tusche M, Kutzsche J, Reiß K, Gremer L, Nagel-Steger L, Willbold D.
Increase of Positive Net Charge and Conformational Rigidity Enhances the Efficacy of d-Enantiomeric Peptides Designed to Eliminate Cytotoxic Aβ Species.
ACS Chem Neurosci. 7 (8), 1088–1096 (2016)
http://pubs.acs.org/doi/abs/10.1021/acschemneuro.6b00047
- Brener O, Dunkelmann T, Gremer L, van Groen T, Mirecka EA, Kadish I, Willuweit A, Kutzsche J, Jürgens D, Rudolph S, Tusche M, Bongen P, Pietruszka J, Oesterhelt F, Langen K-J, Demuth H-U, Janssen A, Hoyer W, Funke SA, Nagel-Steger L, Willbold D
QIAD assay for quantitating a compound's efficacy in elimination of toxic Aβ oligomers.
Sci Rep 5, 13222 (2015)
http://dx.doi.org/10.1038/srep13222
- Jiang N, Leithold LH, Post J, Ziehm T, Mauler J, Gremer L, Cremer M, Schartmann E, Shah NJ, Kutzsche J, Langen KJ, Breitkreutz J, Willbold D, Willuweit A
Preclinical Pharmacokinetic Studies of the Tritium Labelled D-Enantiomeric Peptide D3 Developed for the Treatment of Alzheimer´s Disease
PLoS One 10, e0128553 (2015)
- Pattky M, Nicolardi S, Santiago-Schübel B, Sydes D, van der Burgt YE, Klein AN, Jiang N, Mohrlüder J, Hänel K, Kutzsche J, Funke SA, Willbold D, Willbold S, Huhn C
Structure characterization of unexpected covalent O-sulfonation and ion-pairing on an extremely hydrophilic peptide with CE-MS and FT-ICR-MS.
Anal. Bioanal. Chem. 407, 6637-6655 (2015)
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