- Commercial production of α-N-methylated peptides.
- Modification of the pharmacological profile of therapeutic peptides.
- Use in imaging tumors, discovery of cancer-specific imaging agents.
Key Benefits & Differentiators
- Simpler engineering: Requires fewer chemical steps, enzymes, and overall components for α-N-methylation of peptides.
- Higher Yield: Since it avoids chemical synthesis steps that produce low yields.
- Amenable to rapid genomic changes in substrate peptides.
- Reduces off-target modifications.
Novel method for α-N-methylation of peptides
Although there are significant benefits with efficient drug design, there is still a lack of methods available to easily increase the pharmacological properties of peptides. This directly impacts the efficiency of drug design. Natural products, such as cyclosporin, contain multiple N-methylated peptide bonds and have extremely useful biological traits, such as stability, membrane permeability, target selectivity, affinity, and oral bioavailability. However, due to difficult synthesis processes and the inability to selectively methylate peptides, this approach has rarely been used. This poses limitations to easily creating efficient drugs.
Prof. Michael F. Freeman at the University of Minnesota has developed a technology that improves peptide drug design and creates efficient drugs. This technology is based on a newly discovered natural product called borosins, which contain alpha-N-methylated backbones that are installed through an autocatalytic enzyme. Such N-methylated peptides have desirable pharmaceutical and pharmacological characteristics including improved metabolic stability, membrane permeability, target selectivity, affinity, and oral bioavailability. The engineering and synthesizing of α-N-methylated peptides using this method is simpler since it requires fewer chemical steps, enzymes, and overall components. Additionally, the method also reduces off-target modifications. This technology introduces a system to specifically and efficiently create α-N-methylated peptides for commercial and academic use in a more controlled manner. It provides a starting place for engineering precursor peptide sequences for the production of differentially α-N-methylated peptides. This technology would be beneficial in peptide drug design as it paves the way for the creation of efficient drugs.
Phase of Development
In the process of characterizing the methylation sites, will go into in-vitro testing.
This technology is now available for:
- Sponsored research
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Michael F. Freeman, Ph.D.Biochemistry, Molecular Biology, and Biophysics
Name: Sandipan Banerjee