Streamlined Functionalisation of Nitrogen-containing Molecules by Palladium-catalysed C-H Activation

Informations projet

ACTPD

N° de convention de subvention: 747600

DOI

10.3030/747600

Projet clôturé

Date de signature de la CE 22 Février 2017

Date de début 10 Mars 2017

Date de fin 19 Avril 2019

Financé au titre de

• EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions

Coût total

€ 183 454,80

Contribution de l’UE

€ 183 454,80

Coordonné par

THE CHANCELLOR MASTERS AND SCHOLARS OF THE UNIVERSITY OF CAMBRIDGE
United Kingdom

Periodic Reporting for period 1 - ACTPD (Streamlined Functionalisation of Nitrogen-containing Molecules by Palladium-catalysed C-H Activation)

Période du rapport: 2017-03-10 au 2019-03-09

Résumé du contexte et des objectifs généraux du projet

Chemical reactions are highly valuable tools for scientists and for society since they provide useful materials not found in nature. The overall objective of the project is to develop novel chemical reactions for the synthesis of nitrogen-containing chemicals. This class of substances are vital for human health since they are commonly found in pharmaceuticals. Despite the advancements made in medical science over the past several decades, there is still a lack of effective treatment for many diseases. To meet the pressing demand for new cures, more facile syntheses of biologically active compounds are required. To this end, this project aimed to streamline the synthesis of nitrogen-containing molecules through the development of novel chemical reactions.

Travail effectué depuis le début du projet jusqu’à la fin de la période considérée dans le rapport et principaux résultats atteints jusqu’à présent

A novel chemical reaction for the modification of proteins and peptides, a class of nitrogen-containing compounds, is developed. The reaction makes a structural change to existing proteins or peptides and thus provides a method for obtaining novel biologically active compounds. While proteins and peptides are highly complex compounds, the reaction is highly selective for a specific part of their structure, affording well-defined products. The mild reaction conditions used are also an important feature because proteins and peptides are prone to decomposition. Publication in a high impact journal is expected to publicize this novel reaction, allowing its application in both academia and industry.

Progrès au-delà de l’état des connaissances et impact potentiel prévu (y compris l’impact socio-économique et les conséquences sociétales plus larges du projet jusqu’à présent)

Despite many existing protocols for protein and peptide modification, the reaction developed selectively transforms proteins and peptides in a way that cannot be currently achieved. Therefore, it is expected to find applications in biochemistry and medicinal chemistry. For instance, it may be applied to probe how a protein or peptide carries out its functions in the human body. Such investigations will be important for understanding the cause of certain diseases and for enabling the development of new cures. In addition, the reaction developed can be applied to transform proteins or peptides which are currently used as drugs. The change in structure induced by this reaction could lead to an improvement in pharmacological properties, such as increased potency and reduced side effects. In summary, the outcome of the project could have broad implications in the forefront of biological and medical research.

Protein and Peptide Modification