Peptide Aptamer Technology Aids New Drug Discovery

(Menlo Park, CA, USA) and Aptanomics SA (Lyon, France).

Nanosyn will offer its libraries of small organic compounds, while Aptanomics will use its proprietary peptide aptamer technology to screen those compounds and to characterize any that have promising qualities. Peptide aptamers are artificial recognition molecules whose design is based on the structure of antibodies. They consist of a variable peptide loop attached at both ends to a protein scaffold. This double structural constraint greatly increases the binding affinity of the peptide aptamer to levels comparable to that of an antibody.

Peptide aptamers are selected from an initial pool of around 10 million for their ability to bind the desired target, using proprietary yeast two-hybrid technologies. Each selection identifies a panel of aptamers that "interrogate” the surface of the target protein. Certain aptamers inhibit the biologic function of the target either allosterically or by disrupting a specific protein interaction by direct competition.

Since selection occurs in an intracellular environment where the target is more likely to assume its native three-dimensional conformation, the selected peptide aptamer molecules retain their binding capacity when expressed in cellular or animal models and will not be toxic. Peptide aptamers show high specificity for their target protein, being able to discriminate between closely related proteins or even between different allelic forms of a given protein.

Peptide aptamers may be used to reveal new druggable sites on therapeutic targets, map the sites on the targets, profile the biological effect of intervention at the sites, and to directly identify and develop small molecule antagonists that bind to the desired sites.

Dr. Michael Courtney, CEO of Aptanomics, said, "The fact that Nanosyn believes our technology will successfully identify new druggable sites is an excellent endorsement of our technology. This is a great opportunity to combine our expertise in the identification of new druggable sites and in screening assays for small molecule antagonists with Nanosyn's recognized excellence in medicinal chemistry.”



Related Links:
Aptanomics SA
Nanosyn Inc.