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Research & Development
Bioactive Peptides
Peptides are short proteins formed by a chain consisting of 50 or less amino acids. One of the great strengths of peptides as potential therapies is in the powerful new approaches for discovering and screening new drug candidates.
Peptides have a broad range of potential clinical benefits, with applications in some of the most dire and prevalent disease categories.
The potential applications for peptide therapies are very high: until now, nine products based on peptides are already on the market and over 100 companies are working on new peptides products, many of which are in the late stage clinical trials.
Many efforts have been devoted in the last decade to the development of therapeutic agents based on peptides. The reason for this interest arises from the continuous discovery of new, highly-potent, biologically active peptides. Combinatorial chemistry has contributed greatly in this context. The major limitation in the use of peptides as drugs, such as bio-availability, life time, is in large extent related to the conformational flexibility of the bioactive peptides.
To address this problem, Primm developed the approach of constraining the conformation of peptides to the bioactive one, called "bioactive peptide".
The term bioactive peptides is used to identify molecules of peptidic nature or origin which display a biological behaviour or activity which can be developed at the industrial level for pharmaceutical, diagnostic, chemical and agro-food applications. In this way it is possible to obtain modified peptides with superior properties for therapeutic applications.
The great advantage of using modified peptides instead of classical peptidomimetics is a very high bioavailability, a long lasting activity in vivo, and limited toxicity. Beside this, the costs for setting-up the synthetic strategy are quite low, when compared to those of setting-up stereo-specific synthetic routs.
The strategy adopted by Primm follows these steps:
1) identification of the smallest sequence that causes a measurable biological effect; this is achieved by the synthesis and testing of fragments of the starting peptide sequence;
2) identification of the bioactive conformation, by structure determination and structure-activity relationship studies;
3) peptide design to constrain the conformation, by computer assisted molecular design;
4) chemical synthesis;
5) biological and pharmacological evaluation;
optimisation through iteration of steps 3-5.
Step 3) and 4) can be implemented with an additional step of positional scanning library. A follow-up through the pre-clinical and clinical phases is also performed to overcome unpredictable and undesirable side effects.
Primm is exploiting the existing know-how in peptide chemistry for the development, manufacturing and marketing of proprietary peptides for applications in selected therapeutic areas, with the following objectives:
design of novel peptide molecules for application in the area of HIV entry into the target cells;
development of novel neurokinins antagonists;
modification of existing molecules to improve their pharmacological profile in terms of bio availability and expanding their potential route of administration;
create analogs of the existing molecules of non-peptidic origin. |
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