Objective
This project will contribute towards the molecular design of analogues of transition state structures associated with the degradation of therapeuticals. It will train an essentially computational chemist in experimental techniques, allowing her to become an independent research with broad experience in isotopic studies. The specific experimental training objective of the project is the determination of kinetic isotope effects to interpret the reaction mechanisms of degradation. This will require the synthesis of isotopically-labelled target compounds and the study of their metabolism in vitro in mammalian and bacterial cell cultures. The project is an integral part of a programme researching the molecular mechanisms associated with the metabolism of therapeutic agents and their improvement through enhanced stability. It will focus on nicotine- and tropine-based compounds that are currently medicaments or are in evaluation as potential medicaments. These have a wide range of therapeutic activities: control of tobacco dependency; alleviation of addiction; treatment of neurodegenerative diseases; muscle relaxants. Instability of bioactive compounds presents a serious problem in drug design. The response adopted is frequently the use of higher doses, often associated with deleterious side-effects. A better understanding of the pharmacokinetics can allow a lower dose to be prescribed. Degradation often involves a dominant role for cytochrome P450-dependent oxidases through N-demethylation, oxidation, or ring cleavage. Improved resistance by structural modification or the use of a specific inhibitor will lead to improved therapy. The Host Laboratory has a strong experience in the experimental determination of isotopes in natural products by mass and NMR spectrometries. Acquiring these skills will complement the established abilities of the Researcher in the molecular modelling of reaction intermediates and transition states by in silico calculations of isotope effects.
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: The European Science Vocabulary.
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: The European Science Vocabulary.
- medical and health sciences basic medicine pharmacology and pharmacy pharmaceutical drugs
- medical and health sciences basic medicine medicinal chemistry
- natural sciences chemical sciences electrochemistry electrolysis
- medical and health sciences basic medicine pharmacology and pharmacy pharmacokinetics
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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.
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.
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.
FP7-PEOPLE-2007-2-1-IEF
See other projects for this call
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.
Coordinator
75794 PARIS
France
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.