Peptides are chemical compounds with many medical and industrial applications. They can be used to obtain new materials, as well as drugs or sensors. Also, they can be used as mini-enzymes, in environmentally friendly processes.
Peptides are composed of amino acids and can be compared to necklaces constituted by many beads. In order to improve the biological or catalytic activity of a peptide, collections of analogues are prepared, its activity is tested and the most active ones are selected. Repeating this selection process several times, chemical and pharmaceutical companies can develop products with more potency and selectivity.
Figure 1: Peptides are composed of amino acids and can be compared to necklaces constituted by many beads. Until now, to create them, every analogue is prepared 'de novo', like making every necklace bead by bead. This is a time- and materials-consuming process. Therefore, it would be preferable to develop a method to selectively modify a residue of the chain without affecting the other.
Until now, to make these collections every analogue is prepared de novo, like making every necklace bead by bead. This is a time- and materials-consuming process. Therefore, it would be preferable to develop a method to selectively modify a residue of the chain without affecting the other (figure 1).
Nevertheless, selective modification of peptides is a difficult issue, comparable to changing only one bead in the necklace without touching the others. Although much progress has been made and some special “customizable” units have been created, many problems remain: among them, the difficulty of modifying one customizable unit if several similar units are present, and the preparation of optically pure products.
Scientists at CSIC's Instituto de Productos Naturales y Agrobiología (IPNA) have obtained a customizable unit which can be selectively modified in the presence of natural amino acids and other convertible units, affording optically pure products. It can be transformed into a wide variety of derivatives and offers the possibility of obtaining products “à la carte”. Therefore, from only one or a few peptides, a diversity of derivatives and product libraries can be obtained.
Figure 2. Many compounds with high commercial value can be obtained by scission and modification of the convertible unit (in red and blue). From left to right, components of branched peptides and medical probes, homoserine lactones and lactams, valuable N-methyl or N-alkyl amino acids, and peptides with non natural units.
The convertible unit and the process developed by the CSIC scientists are highly versatile. As the figure 2 shows, many compounds with high commercial value can be obtained by scission and modification of the convertible unit (in red and blue). From left to right, components of branched peptides and medical probes, homoserine lactones and lactams, valuable N-methyl or N-alkyl amino acids, and peptides with non natural units.
No less important is that a few milligrams of these commercial compounds can cost up to hundreds of Euros. On the contrary, this new process enables the obtention of highly optical pure products at a substantially lower cost.
This new technology has been patented. Pharmaceutical and biotechnological partners interested in developing and commercializing applications of these compounds are sought.
Contact:
Andrés Borges
Unidad de Transferencia del Conocimiento
Instituto de Productos Naturales y Agrobiología (IPNA)
E-mail:
Tel. 922 256 847 ext. 234