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Peptides for the Diagnosis and Therapy of Alzheimer’s Disease

Reference Number TO 11-00011

Challenge

Current scientific research in the field of Alzheimer’s Disease (AD) focuses on the identification of Abeta plaque precursor fibrils, their occurrence in diseased brains and amyloid plaques, and their role in the pathogenic processes. A strong need is felt for therapeutics, but also for means for detection of amyloid plaques during disease stages without or only minor onset of AD symptoms. Such diagnostic tools are also of importance for monitoring the disease progression and therapy effects in a non-invasive way.

Reduction of Abeta plaque load in transgenic mice upon 30 days in brain infusion D3. a) saline, b) D1-peptide, c) D3-peptide. van Groen, 2008.
Reduction of Abeta plaque load in transgenic mice upon 30 days in brain infusion D3. a) saline, b) D1-peptide, c) D3-peptide. van Groen, 2008.

Technology

The technology relates to synthetic D-Peptides, specific for Abeta 42 amyloid plaques and highly affine with an in vitro KD in the submicromolar range. Evidence for in vivo binding was given by histological analysis of transgenic mice brain tissues. Two D-peptides D1 and D3 were functionally tested in AD transgenic mice models.
Upon intracranial administration, in vivo plaque specificity of D1 could be confirmed, without brain inflammation or uptake by astrocytes or microglia even after long-term infusion and in good correlation to results from cellular cytotoxicity assays. D1 may therefore be suitable for measuring plaque load in the living brain for early onset of the disease, and monitoring of plaque load during disease progression and treatment.
D3 reduces the amyloid plaque load in transgenic mice after a 4 weeks intracranical infusion. Upon oral administration the cognitive behaviour of treated mice improved, making D3 to a promising candidate molecule for therapeutic purposes. 
Current preliminary data indicate the passage of the blood brain barrier for both peptides.

Commercial Opportunity

In-licensing and collaboration opportunity.

Patent Situation

A  European Patent is granted (EP 1379546).

Further Reading

  • Funke et al., ACS Chem. Neurosci. 2010, 1, 639-648
  • Van Groen et al., ChemMedChem 2009, 4, 276-282
  • Van Groen et al., ChemMedChem 2008, 3, 1848-1852
  • Wiesehan et al., Protein Engineering, Design & Selection, 21 (4), 241-246
  • Wiesehan et al., ChemBioChem 2003, 4, 748-753