Manus Pharmaceuticals is focused on developing novel small peptide therapeutics.
A peptide consists of two or more amino acids joined by peptide bonds. Peptides work by binding to activation sites on receptors. This binding can allow for the prevention or enhancement of the body’s processes. Peptides provide an added advantage over other biologics because of their small size, lack of immunogenicity, and the ease with which the body processes them. Proteins and antibodies are generally associated with worse side effects than are peptides, and with more difficult delivery. The body sees monoclonal antibodies and foreign proteins as antigens, and the immune system will respond to them. This often creates rebound problems or severe reactions. Short peptides are not immunogenic and therefore avoid these issues.
Manus Pharmaceuticals has developed a unique two-stage approach to the creation of peptide drugs. In stage I, biologically active peptides were isolated from different organs and tissues. In stage II, the peptides were synthetically reproduced, replicating the structure and properties of the isolated natural molecules. The structural and functional interactions of biologically active peptides were studied and the most promising structures were chosen for further development of potential drugs. This approach can be described as a “functionally selective” approach to drug development. With traditional approaches, only one in 5,000 compounds developed in the laboratory will reach clinical testing in human subjects. The functional selective approach allows one in 100 compounds developed in the laboratory to reach clinical testing. This approach creates dramatic savings in time, cost and risk undertaken to successfully develop a new drug.
When Dr. Deigin studied analogs of immuno- and neuropeptides, he detected patterns relating to the targeted synthesis of natural peptide analogs. Dr. Deigin believes that potential medical applications may be developed through the application of specific chemical and biological properties associated with these two large classes of compounds. This discovery provides the Company with a wealth of future potential drug candidates to be utilized as it grows.
- PEPTIDE CHEMISTRY
1.1. Structural and Functional Studies of Peptides
The scientific interests of Manus Pharmaceuticals are focused on structural and functional interactions of biologically active peptides.
When studying new analogs of two main classes of compounds as an immuno – and neuropeptides, some regularity were found for targeted synthesis of natural peptide analogs with specific chemical and biological properties allowing their potential medical use.
1.2. Methods of Laboratory Synthesis.
Manus Pharmaceuticals employs modern equipment for classic and solid-phase peptide synthesis and can effectively develop optimal laboratory methods for synthesis of peptides of any length and complexity.
Depending on necessary properties the peptide will be either obtained by the solid-phase method or synthesized in solution. In any case, the scheme of synthesis will be elaborated individually, to fit the specific features of the peptide amino acid sequence.
1.3. Methods of Analysis and Purification
All synthesized peptides undergo a thorough purification by preparative HPLC. Our scientists have designed a proprietary preparatory chromatographic column. It allows for effective and rapid preparative purification of peptides.
Our Analytical Laboratory has developed and uses the latest physico-chemical methods to analyze synthesized peptides. In the Analytical Laboratory we use amino acid analysis, MS-HPLC, HPLC, gas chromatography, NMR, UV and mass- spectroscopy.
1.4. Technology of Industrial Peptide Synthesis
The results of structural and functional studies help choose the most promising peptide from the point of view of creating a pharmaceutical product. Having regard to the specific features of a given structure the specialists of the Technological Department elaborate the most convenient and economical production scheme and synthesize pilot amounts of the preparation for laboratory tests. If the preparation is found to be promising, the Technological Department develops experimental commercial technology of the peptide production. By now, production technologies have been developed for the peptide preparation “STVOLOGEN”.
- Deigin V. I. “Branched piperazin-2,5–dion derivatives (2,5-DKP) of peptides and small molecules”. РСТ: “Multifunctional Bioactive Compounds”. WO 2008/014613 -1-PCT/CA2007/001357.
- Deigin V. I. “Multifunctional bioactive compounds.” European Patent # 2046778. Priorities Date 01.08. 2007.
- Deigin V. I. “Multifunctional bioactive compounds.” Canadian Patent # 2,659,875. Priorities Date 01.08. 2007.
- Deigin V. I. “Substituted Piperazin-2,5-diones As multifunctional Bioactive Compounds.” USA Patent # 9,108,931B2. Priorities Date 01.08. 2007.
- Deigin V. I. “Multifunctional bioactive compounds.” Japanese Patent # 5357022. Priorities Date 01.08. 2007.
- Deigin V. I. “Multifunctional bioactive compounds.” Eurasian Patent # 018548. Priorities Date 01.08. 2007