Project description DEENESFRITPL A microreactor for novel peptide functionalisation could spur greener drug discovery Site-selective modification of proteins or peptides has become a very common strategy to modulate protein function. Addition of a sulfonyl group to lysine, an amino acid that is a constituent of most proteins, is of growing interest to the research community as it could open the door to new possibilities for targeted therapies. Electrosynthesis, particularly for oxidation-reduction reactions involving electron transfer between species, has gained renewed attention as a greener synthesis method within the energy-intensive chemical industry. ELECTROSULF is exploiting the technology in a flow microreactor for oxidative sulfonylation of lysine, creating a new eco-friendly way to functionalise peptides and spur new drug discovery. Show the project objective Hide the project objective Objective Peptides are important molecules, ubiquitous in biological systems. Their relevance in the pharmaceutical sector is proven by the constant increase which the global market of peptide-based drugs is experiencing in the last years. As a consequence, several methods have been developed to modify peptides (e.g. condensation, cross-coupling, transition-metal catalysis, and photocatalysis), being lysine with its free amine one of the most preferred handles used by chemists to introduce a new moieties, e.g. cytotoxic drugs or fluorescent labels. Several transformations as alkylation, arylation, oxidation, acylation and condensation have been described for lysine. However, it would be very appealing to introduce selectively a sulfonyl group, which would result in the formation of a sulfonamide, a functionality which is widely employed in drugs. Although several oxidative sulfonylations are reported in the literature, their drawbacks motivate me to look for greener synthetic strategies. Electrosynthesis represents an advantageous alternative, which has been re-discovered in the last years also thanks to its employment in continuous-flow microreactors. With the support of this modern technology, it is possible to minimize the difficulties connected to older electrochemical processes (such as mass-transfer limitation, the need of a supporting electrolyte,and the difficult scale-up). ELECTROSULF aims at developing a novel sulfonylation of lysine by electrochemical means with the use of a flow microreactor. The reaction mechanism will be also properly studied. My strong background in organic chemistry together with Prof. Timothy Noël’s expertise in flow processes and reaction miniaturization will guarantee the success of ELECTROSULF, whose achievement will have a great impact on the pharmaceutical sector, paving the path to a new approach for peptide modification. Fields of science natural scienceschemical sciencescatalysisphotocatalysismedical and health sciencesbasic medicinepharmacology and pharmacypharmaceutical drugsnatural scienceschemical scienceselectrochemistryelectrolysisnatural sciencesbiological sciencesbiochemistrybiomoleculesnatural scienceschemical sciencesorganic chemistryamines Programme(s) H2020-EU.1.3. - EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions Main Programme H2020-EU.1.3.2. - Nurturing excellence by means of cross-border and cross-sector mobility Topic(s) MSCA-IF-2018 - Individual Fellowships Call for proposal H2020-MSCA-IF-2018 See other projects for this call Funding Scheme MSCA-IF-EF-ST - Standard EF Coordinator TECHNISCHE UNIVERSITEIT EINDHOVEN Net EU contribution € 175 572,48 Address Groene loper 3 5612 AE Eindhoven Netherlands See on map Region Zuid-Nederland Noord-Brabant Zuidoost-Noord-Brabant Activity type Higher or Secondary Education Establishments Links Contact the organisation Opens in new window Website Opens in new window Participation in EU R&I programmes Opens in new window HORIZON collaboration network Opens in new window Other funding € 0,00
