Objective
Fragment-based ligand discovery (FBLD) has become a mainstream strategy to discover new drugs to enable the treatment of conditions with unmet medical needs. Despite the remarkable rise of FBLD, significant chemical challenges remain in the field; firstly, elaborated fragments tend to be synthesised de novo when direct growth would be much more advantageous. Secondly, the currently available toolkit for fragment elaboration tends to exacerbate an uneven exploration of chemical space, yielding flatter and more lipophilic compounds.
SYNFOS will allow Alexandre Trindade (the fellow) to join the laboratory of Professors Adam Nelson (host supervisor) and Steve Marsden (host co-supervisor) at the University of Leeds (Host) and develop research expertise in fragment-based ligand discovery; catalysis to enable molecular discovery; protein-protein interaction (PPIs) inhibition; and high-throughput X-ray crystallography (via secondments to Diamond (Partner)). In doing so, the fellow will (a) enhance his prospects of becoming an independent academic group leader in Europe and (b) address the need to train researchers in key multidisciplinary areas such as medicinal chemistry and chemical biology and (c) develop cutting edge synthetic methods that facilitates the fragment-based discovery of new inhibitors for protein-protein interactions. By building in fragment hits from the Host laboratory, the fellow will establish a synthetic toolkit enabling the functionalization of C-H bonds within N-heterocycles with a wide range of medicinally-relevant groups. The fellowship will explore three main modes of reactivity to establish the functionalization of sp3-hydridised carbons with heterocyclic fragments and showcase the value of the synthetic toolbox through the discovery of fragments hits into potent inhibitors of PPIs involving the ATAD2 bromodomain.
Fields of science (EuroSciVoc)
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: https://op.europa.eu/en/web/eu-vocabularies/euroscivoc.
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: https://op.europa.eu/en/web/eu-vocabularies/euroscivoc.
- medical and health sciences basic medicine pharmacology and pharmacy drug discovery
- natural sciences biological sciences biochemistry biomolecules proteins proteomics
- medical and health sciences basic medicine medicinal chemistry
- natural sciences earth and related environmental sciences geology mineralogy crystallography
- natural sciences chemical sciences catalysis
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Keywords
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Programme(s)
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
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H2020-EU.1.3. - EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions
MAIN PROGRAMME
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H2020-EU.1.3.2. - Nurturing excellence by means of cross-border and cross-sector mobility
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Topic(s)
Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.
Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.
Funding Scheme
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
MSCA-IF - Marie Skłodowska-Curie Individual Fellowships (IF)
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Call for proposal
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
(opens in new window) H2020-MSCA-IF-2017
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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.
LS2 9JT Leeds
United Kingdom
The total costs incurred by this organisation to participate in the project, including direct and indirect costs. This amount is a subset of the overall project budget.