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Receptor Ligand Peptidomimetics
The Company’s technology is based on more than 10 years of research into the design of small molecules, which mimic the activity of natural ligands.
Many protein-protein interactions occur via contact at a small number of key regions, so-called Hot Spots, rather than extensive interactions over the whole protein surface. The interactions generally involve up to 30 contact side chains on discontinuous portions of each primary sequence of the protein. However, only a small percentage of these side-chains are required for tight binding. Small molecules that interact with these hot spots can interfere with the normal protein-protein interactions, making the concept of ligand mimicry viable. Extensive studies have shown that some of the hot spots are localized in the turn regions of proteins.
Scientific Approach
Generally there are two approaches for the development and design of small molecule ligands to receptors, both involving molecular design and peptidomimicry.
In the case of the company's neurotrophin (NTF) receptors, that starting point was the design of structural analogs. Hot spots relevant for binding and function could be predicted by utilizing available structural data, site directed mutagenesis and recombinant NTF chimeras with mimetics of the hot spots yielding receptor-selective ligands.
Antibody mimicry is an alternative technology that often produces both ligand mimics that not only bind specifically, but also exhibit functionality.
Company Ocular Disease Targets
Mimetogen has targeted a number of well-validated cell surface neurotrophin receptor markers that represent potential targets for the development of small molecules, which mimic the highly specific action of the natural receptor ligands, which have been implicated in several ocular indications of both the anterior and posterior segments of the eye.
Drug Linker Technology
In addition to the broad portfolio of novel compounds, Mimetogen has developed a proprietary drug-linker technology, which can be used in conjunction with many different targeting ligands and effector drugs.
In vivo validation studies have shown that the drug-linker technology can be used to increase the therapeutic index of known anti-cancer therapeutics by more than 400-fold while exhibiting absolutely no increase in toxicity.
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1000 de La Gauchetière Street West, Suite 900. Montréal, Québec, H3B 5H4, Canada
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