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Engineering new enzymatic platforms for atroposelective C–N bond formation

Project description

Engineering enzymes for sustainable synthesis of axially chiral drug molecules

Controlling a molecule’s three-dimensional shape is essential for its physical and biological properties. Atropisomers, which possess axial chirality due to hindered bond rotation, influence pharmacological outcomes. However, their selective synthesis remains a challenge in drug development. Current methods often rely on inefficient chromatographic separations. Supported by the Marie Skłodowska-Curie Actions Programme, the AtropEnzymes project will engineer enzymes for novel, atroposelective C–N bond-forming reactions. Using directed evolution, machine learning and computational design, this research aims to establish a sustainable biocatalytic framework for the efficient production of medicinally relevant, axially chiral compounds.

Objective

The control of a molecule’s three-dimensional shape has important implications for both its physical and biological properties. Atropisomers—stereoisomers resulting from hindered rotation around a single bond—exhibit axial chirality that can profoundly impact pharmacological properties, making their selective synthesis increasingly important in drug development. Although the number of single-atropisomer pharmaceuticals has significantly grown over the past decade, methods for their stereoselective preparation remain limited, with inefficient and costly chromatographic separations still widely used. This project addresses this challenge by engineering enzymes capable of novel atroposelective C–N bond-forming reactions, providing direct access to medicinally relevant axially chiral scaffolds. The approach will combine enzymatic desymmetrisation to access electron-rich biaryl atropisomers with atroposelective SNAr reactions to generate electron-poor counterparts. Directed evolution will be applied to enhance activity and selectivity, supported by machine learning to accelerate optimisation and computational protein design to improve enzyme function. Together, these studies will establish a biocatalytic platform for the efficient, sustainable synthesis of drug-like atropisomeric compounds.

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HORIZON-TMA-MSCA-PF-GF - HORIZON TMA MSCA Postdoctoral Fellowships - Global Fellowships

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Coordinator

THE UNIVERSITY OF MANCHESTER
Net EU contribution

Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.

€ 355 301,04
Address
OXFORD ROAD
M13 9PL Manchester
United Kingdom

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Region
North West (England) Greater Manchester Manchester
Activity type
Higher or Secondary Education Establishments
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Total cost

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