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ISOTOPICS SIGNED

ISOTOPIC LABELING FOR DRUG INNOVATION

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EC-Contrib. €

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Partnership

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 ISOTOPICS project word cloud

Explore the words cloud of the ISOTOPICS project. It provides you a very rough idea of what is the project "ISOTOPICS" about.

identification    pressing    efficient    synthesis    ddd    interdisciplinary    excretion    attrition    techniques    plan    scarcity    taught    biologics    display    occupancy    molecule    therapeutic    inter    radiochemists    experts    timeline    profound    labeled    trials    rates    labeling    issue    strategy    secondments    accelerate    industry    drug    metabolism    earlier    successfully    profile    interactive    beneficial    vivo    critically    innovative    consequently    isotopic    expert    generation    receptor    diseases    isotopics    disciplinary    innovation    solutions    closely    dramatically    combined    engagement    small    training    urgently    chemists    train    huge    pharmaceutical    chemistries    larger    medicinal    radiochemistry    candidates    discovery    revival    drugs    efficacy    pharmacokinetic    clinical    chemistry    absorption    pharmacodynamic    de    risking    class    series    programs    streamline    first    expertise    molecules    lack    evaluation    stage    excessive    isotopically    relationships   

Project "ISOTOPICS" data sheet

The following table provides information about the project.

Coordinator
COMMISSARIAT A L ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES 

Organization address
address: RUE LEBLANC 25
city: PARIS 15
postcode: 75015
website: www.cea.fr

contact info
title: n.a.
name: n.a.
surname: n.a.
function: n.a.
email: n.a.
telephone: n.a.
fax: n.a.

 Coordinator Country France [FR]
 Project website http://www.isotopics-project.eu/
 Total cost 3˙948˙843 €
 EC max contribution 3˙948˙843 € (100%)
 Programme 1. H2020-EU.1.3.1. (Fostering new skills by means of excellent initial training of researchers)
 Code Call H2020-MSCA-ITN-2015
 Funding Scheme MSCA-ITN-ETN
 Starting year 2016
 Duration (year-month-day) from 2016-01-01   to  2019-12-31

 Partnership

Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 
1    COMMISSARIAT A L ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES FR (PARIS 15) coordinator 1˙051˙502.00
2    THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD UK (OXFORD) participant 1˙093˙151.00
3    KAROLINSKA INSTITUTET SE (STOCKHOLM) participant 527˙318.00
4    ASTRAZENECA AB SE (SODERTAELJE) participant 263˙659.00
5    CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS FR (PARIS) participant 262˙875.00
6    UCB BIOPHARMA SRL BE (BRUXELLES) participant 250˙560.00
7    UNIVERSITE DE LIEGE BE (LIEGE) participant 250˙560.00
8    SANOFI-AVENTIS DEUTSCHLAND GMBH DE (FRANKFURT AM MAIN) participant 249˙216.00
9    UCB PHARMA SA BE (BRUXELLES) participant 0.00
10    INSTN FR (Saclay) partner 0.00
11    LERMIT FR (Chatenay-Malabry) partner 0.00
12    Société de Chimie Thérapeutique FR (Chatenay-Malabry) partner 0.00
13    UNIVERSITE PARIS-SUD FR (ORSAY CEDEX) partner 0.00

Map

 Project objective

Excessive attrition rates during clinical trials dramatically impact on Drug Discovery and Development (DDD). Absorption, Distribution, Metabolism and Excretion studies carried out on larger series of drug candidates at an earlier stage of the DDD timeline and evaluation of drug efficacy through better assessment of pharmacokinetic/pharmacodynamic relationships, target engagement and receptor occupancy are critically important approaches for de-risking drug innovation since they facilitate early identification of the candidates that display the best in vivo profile. When successfully implemented, this strategy can accelerate the discovery of new therapeutic solutions to existing and emerging diseases, and enhance European pharmaceutical innovation. For implementation, large sets of isotopically-labeled molecules are required and consequently, a huge revival of labeling techniques is urgently needed. Another crucial issue is the scarcity of expert radiochemists in Europe and the lack of first class training programs in this inter-disciplinary field merging chemistry, radiochemistry and medicinal chemistry. The aims of ISOTOPICS are: i) to train the next generation of European chemists with expertise in isotopic labeling and advanced medicinal chemistry through a first-class taught and research training program combined with a highly interactive secondments plan; ii) to develop innovative and general isotopic labeling chemistry and radiochemistry to streamline the synthesis of labeled small-molecule drugs and biologics; iii) to work closely with the European pharmaceutical industry to apply the new labeling methods to drugs currently in development in order to provide solutions to the most pressing problems in drug innovation. This highly interdisciplinary project is expected to have a profound beneficial impact on drug innovation in Europe by providing novel efficient techniques and new experts in the fields of labeling and medicinal chemistries.

 Deliverables

List of deliverables.
Network-wide Periodic Network meetings Other 2020-03-27 09:15:34
Cascade reactions to construct 14C-heterocycles and derivatizing peptides and proteins from K14CN Documents, reports 2020-03-27 09:17:10
N-Methylation/C-carbonylation from CO2 for the [14C]radiolabeling of small-molecule drugs Documents, reports 2020-03-27 09:17:17
Cu(III)-catalyzed [18F]fluorination of arenes and heteroarenes Documents, reports 2020-03-27 09:17:25
Development of new hydrophilic and air-resistant RuNps for [2H/3H]labeling of drugs & biologics Documents, reports 2020-03-27 09:15:19
New methods for [2H/3H]labeling of small molecules drugs and peptides Documents, reports 2020-03-27 09:15:11
Scientific meeting reports Documents, reports 2020-03-27 09:16:45
Dissemination of main results Other 2020-03-27 09:16:28
Development, evaluation and applications of new methods for asymmetric [18F]fluorination Documents, reports 2020-03-27 09:17:36
New methods for [2H/3H]labeling of biologics Documents, reports 2020-03-27 09:17:02
Defence of PhD Thesis Documents, reports 2020-03-27 09:16:12
Development of a novel automated radio-chemistry system for [11C]carbonylation Documents, reports 2020-03-27 09:14:49
Training in information technology skills Documents, reports 2020-03-27 09:15:25
Microfluidic [11C]carbonylation screening under radical initiated conditions Documents, reports 2020-03-27 09:14:35
Results dissemination Documents, reports 2020-03-27 09:15:57
Development of Suzuki protein chemistry for the [18F]labeling of proteins Documents, reports 2020-03-27 09:17:52
Improvement of employability Documents, reports 2020-03-27 09:16:04
Network-wide interdisciplinary scientific training Websites, patent fillings, videos etc. 2020-03-27 09:15:49
Development of a photochemical flow process for addition of [18F]CHF to (hetero)aromatics Documents, reports 2020-03-27 09:14:28
Development of new fluoro- and difluoromethyl-sulfonyl reagents for the production of [18F]labeled alkenes Documents, reports 2020-03-27 09:17:44
Public Engagement Websites, patent fillings, videos etc. 2020-03-27 09:16:52
Website and Newsletters Websites, patent fillings, videos etc. 2020-03-27 09:16:20
Application of N-methylation and C-carbonylation from CO2 to [11C]labeling Documents, reports 2020-03-27 09:15:04
Patents, research and review publications, assistance for creation of start-ups and incubation Documents, reports 2020-03-27 09:16:37
Supervisory Board of the Network Documents, reports 2020-02-17 17:33:06
Communication and presentation skills Documents, reports 2020-02-17 17:33:24
ESR recruitment process Other 2020-02-17 17:33:23

Take a look to the deliverables list in detail:  detailed list of ISOTOPICS deliverables.

 Publications

year authors and title journal last update
List of publications.
2020 Choon Wee Kee, Osman Tack, Florian Guibbal, Thomas C. Wilson, Patrick G. Isenegger, Mateusz Imiołek, Stefan Verhoog, Michael Tilby, Giulia Boscutti, Sharon Ashworth, Juliette Chupin, Roxana Kashani, Adeline W. J. Poh, Jane K. Sosabowski, Sven Macholl, Christophe Plisson, Bart Cornelissen, Michael C. Willis, Jan Passchier, Benjamin G. Davis, Véronique Gouverneur
18 F-Trifluoromethanesulfinate Enables Direct C–H 18 F-Trifluoromethylation of Native Aromatic Residues in Peptides
published pages: 1180-1185, ISSN: 0002-7863, DOI: 10.1021/jacs.9b11709
Journal of the American Chemical Society 142/3 2020-03-05
2019 Mégane Valero, Donia Bouzouita, Alberto Palazzolo, Jens Atzrodt, Christophe Dugave, Simon Tricard, Sophie Feuillastre, Grégory Pieters, Bruno Chaudret, Volker Derdau
NHC-Stabilized Iridium Nanoparticles as Novel Catalysts in Hydrogen Isotope Exchange Reactions of Anilines
published pages: , ISSN: 1433-7851, DOI: 10.1002/anie.201914369
Angewandte Chemie International Edition 2020-01-28
2019 Mélodie Ferrat, Kenneth Dahl, Christer Halldin, Magnus Schou
“In-loop” carbonylation - a simplified method for carbon-11 labeling of drugs and radioligands
published pages: , ISSN: 0362-4803, DOI: 10.1002/jlcr.3805
Journal of Labelled Compounds and Radiopharmaceuticals 2020-01-14
2019 Malvika Sardana, Joakim Bergman, Cecilia Ericsson, Lee Peter Kingston, Magnus Schou, Christophe Dugave, Davide Audisio, Charles S. Elmore
Visible-Light Enabled Aminocarbonylation of Unactivated Alkyl Iodides with Stoichiometric Carbon Monoxide for Application on Late-Stage Carbon Isotope Labeling
published pages: , ISSN: 0022-3263, DOI: 10.1021/acs.joc.9b02575
The Journal of Organic Chemistry 2019-12-16
2019 Juan M. Asensio, Donia Bouzouita, Piet W. N. M. van Leeuwen, Bruno Chaudret
σ-H–H, σ-C–H, and σ-Si–H Bond Activation Catalyzed by Metal Nanoparticles
published pages: , ISSN: 0009-2665, DOI: 10.1021/acs.chemrev.9b00368
Chemical Reviews 2019-11-18
2019 Kaisa Horkka, Kenneth Dahl, Jonas Bergare, Charles S. Elmore, Christer Halldin, Magnus Schou
Rapid and Efficient Synthesis of 11 C-Labeled Benzimidazolones Using [ 11 C]Carbon Dioxide
published pages: 1846-1849, ISSN: 2365-6549, DOI: 10.1002/slct.201803561
ChemistrySelect 4/6 2019-10-15
2018 Ryan A. Bragg, Malvika Sardana, Markus Artelsmair, Charles S. Elmore
New trends and applications in carboxylation for isotope chemistry
published pages: 934-948, ISSN: 0362-4803, DOI: 10.1002/jlcr.3633
Journal of Labelled Compounds and Radiopharmaceuticals 61/13 2019-10-15
2019 Laura Trump, Agostinho Lemos, Bénédicte Lallemand, Patrick Pasau, Joël Mercier, Christian Lemaire, André Luxen, Christophe Genicot
Late-Stage 18 F-Difluoromethyl Labeling of N-Heteroaromatics with High Molar Activity for PET Imaging
published pages: 13149-13154, ISSN: 1433-7851, DOI: 10.1002/anie.201907488
Angewandte Chemie International Edition 58/37 2019-09-26
2019 Mégane Valero, Daniel Becker, Kristof Jess, Remo Weck, Jens Atzrodt, Thomas Bannenberg, Volker Derdau, Matthias Tamm
Directed Iridium‐Catalyzed Hydrogen Isotope Exchange Reactions of Phenylacetic Acid Esters and Amides
published pages: 6517-6522, ISSN: 0947-6539, DOI: 10.1002/chem.201901449
Chemistry – A European Journal 25/26 2019-09-26
2019 Mégane Valero, Anurag Mishra, Jennifer Blass, Remo Weck, Volker Derdau
Comparison of Iridium(I) Catalysts in Temperature Mediated Hydrogen Isotope Exchange Reactions
published pages: , ISSN: 2191-1363, DOI: 10.1002/open.201900204
ChemistryOpen 2019-09-26
2019 Karen Hinsinger, Grégory Pieters
The Emergence of Carbon Isotope Exchange
published pages: , ISSN: 1433-7851, DOI: 10.1002/anie.201905368
Angewandte Chemie International Edition 2019-09-26
2018 Niels Rothermel, Donia Bouzouita, Tobias Röther, Iker de Rosal, Simon Tricard, Romuald Poteau, Torsten Gutmann, Bruno Chaudret, Hans‐Heinrich Limbach, Gerd Buntkowsky
Surprising Differences of Alkane C‐H Activation Catalyzed by Ruthenium Nanoparticles: Complex Surface‐Substrate Recognition?
published pages: 4243-4247, ISSN: 1867-3880, DOI: 10.1002/cctc.201801022
ChemCatChem 10/19 2019-09-26
2019 Agostinho Lemos, Christian Lemaire, André Luxen
Progress in Difluoroalkylation of Organic Substrates by Visible Light Photoredox Catalysis
published pages: 1500-1537, ISSN: 1615-4150, DOI: 10.1002/adsc.201801121
Advanced Synthesis & Catalysis 361/7 2019-09-26
2019 Alberto Palazzolo, Sophie Feuillastre, Viktor Pfeifer, Sébastien Garcia-Argote, Donia Bouzouita, Simon Tricard, Céline Chollet, Elodie Marcon, David-Alexandre Buisson, Sophie Cholet, François Fenaille, Guy Lippens, Bruno Chaudret, Grégory Pieters
Efficient Access to Deuterated and Tritiated Nucleobase Pharmaceuticals and Oligonucleotides using Hydrogen-Isotope Exchange
published pages: 4891-4895, ISSN: 1433-7851, DOI: 10.1002/anie.201813946
Angewandte Chemie International Edition 58/15 2019-09-26
2018 Antonio Del Vecchio, Gianluca Destro, Frédéric Taran, Davide Audisio
Recent developments in heterocycle labeling with carbon isotopes
published pages: 988-1007, ISSN: 0362-4803, DOI: 10.1002/jlcr.3666
Journal of Labelled Compounds and Radiopharmaceuticals 61/13 2019-09-26
2018 Antonio Del Vecchio, Fabien Caillé, Arnaud Chevalier, Olivier Loreau, Kaisa Horkka, Christer Halldin, Magnus Schou, Nathalie Camus, Pascal Kessler, Bertrand Kuhnast, Frédéric Taran, Davide Audisio
Late-Stage Isotopic Carbon Labeling of Pharmaceutically Relevant Cyclic Ureas Directly from CO 2
published pages: 9744-9748, ISSN: 1433-7851, DOI: 10.1002/anie.201804838
Angewandte Chemie International Edition 57/31 2019-09-26
2018 Gabriele Pupo, Francesco Ibba, David M. H. Ascough, Anna Chiara Vicini, Paolo Ricci, Kirsten E. Christensen, Lukas Pfeifer, John Richard Morphy, John M. Brown, Robert S. Paton, Véronique Gouverneur
Asymmetric nucleophilic fluorination under hydrogen bonding phase-transfer catalysis
published pages: 638-642, ISSN: 0036-8075, DOI: 10.1126/science.aar7941
Science 360/6389 2019-09-26
2018 Matthew K. Bilyard, Henry J. Bailey, Lluís Raich, Maria A. Gafitescu, Takuya Machida, Javier Iglésias-Fernández, Seung Seo Lee, Christopher D. Spicer, Carme Rovira, Wyatt W. Yue, Benjamin G. Davis
Palladium-mediated enzyme activation suggests multiphase initiation of glycogenesis
published pages: 235-240, ISSN: 0028-0836, DOI: 10.1038/s41586-018-0644-7
Nature 563/7730 2019-09-26
2018 Philipp Gotico, Antonio Del Vecchio, Davide Audisio, Annamaria Quaranta, Zakaria Halime, Winfried Leibl, Ally Aukauloo
Visible-Light-Driven Reduction of CO 2 to CO and Its Subsequent Valorization in Carbonylation Chemistry and 13 C Isotope Labeling
published pages: 715-719, ISSN: 2367-0932, DOI: 10.1002/cptc.201800012
ChemPhotoChem 2/8 2019-09-26
2019 Gabriele Pupo, Anna Chiara Vicini, David M. H. Ascough, Francesco Ibba, Kirsten E. Christensen, Amber L. Thompson, John M. Brown, Robert S. Paton, Véronique Gouverneur
Hydrogen Bonding Phase-Transfer Catalysis with Potassium Fluoride: Enantioselective Synthesis of β-Fluoroamines
published pages: 2878-2883, ISSN: 0002-7863, DOI: 10.1021/jacs.8b12568
Journal of the American Chemical Society 141/7 2019-09-26
2018 Gianluca Destro, Olivier Loreau, Elodie Marcon, Frédéric Taran, Thibault Cantat, Davide Audisio
Dynamic Carbon Isotope Exchange of Pharmaceuticals with Labeled CO 2
published pages: , ISSN: 0002-7863, DOI: 10.1021/jacs.8b12140
Journal of the American Chemical Society 2019-09-26
2019 Mégane Valero, Volker Derdau
Highlights of aliphatic C (sp 3 )-H Hydrogen Isotope Exchange Reactions
published pages: , ISSN: 0362-4803, DOI: 10.1002/jlcr.3783
Journal of Labelled Compounds and Radiopharmaceuticals 2019-09-26

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