Objective This proposal builds on the proven methodology developed in the SEtTReND FP7 project to develop inhibitors of schistosome HME as lead compounds for new drugs. We will employ a target-based strategy for the development of novel drug leads against schistosomiasis, leishmaniasis, Chagas disease and malaria by targeting histone modifying enzymes (HME), in particular those involved in acetylation/deacetylation and methylation/demethylation. The principal objectives of A-PARADDISE are:- The identification of HMEs from Leishmania sp. and Trypanosoma cruzi and the molecular characterization and functional characterization of selected potential targets,- Phenotypic screening of Leishmania, T. cruzi, S. mansoni and P. falciparum using HME class inhibitors, inhibitors developed specifically against S. mansoni and P. falciparum HMEs. This will permit us to obtain a comprehensive view of inhibitor classes and chemical scaffolds of interest,- Production of recombinant Leishmania and T. cruzi HME proteins, structural studies. Selected, validated target enzymes will be produced, crystallized and analysed by X-ray diffraction. Assays will be optimized to permit testing of inhibitors,- High-throughput and structure-based (in silico) screening of selected HMEs. Inhibitors selected will be further screened by phenotypic assays on the parasites in vitro,- Optimisation of inhibitor structures by chemical synthesis based on molecular modelling studies (inhibitors of all origins),- Transcriptomic analysis of drug-treated parasites to verify target specificity and mechanism of action (all parasites),- Pharmacological and toxicological studies (in vitro and in vivo) of selected inhibitors, in vivo testing of compounds in parasite-infected mice.The overall objective of the A-PARADDISE project is to develop optimized epigenetic inhibitors for further testing and optimisation as drug candidates against the four parasites studied. Fields of science medical and health sciencesbasic medicinepharmacology and pharmacydrug discoverymedical and health scienceshealth sciencesinfectious diseasesmalarianatural sciencesbiological sciencesbiochemistrybiomoleculesproteinsenzymesnatural sciencesbiological sciencesgeneticsepigenetics Programme(s) FP7-HEALTH - Specific Programme "Cooperation": Health Topic(s) HEALTH.2013.2.3.4-2 - Drug development for neglected parasitic diseases Call for proposal FP7-HEALTH-2013-INNOVATION-1 See other projects for this call Funding Scheme CP-FP - Small or medium-scale focused research project Coordinator INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE Address Rue de tolbiac 101 75654 Paris France See on map Region Ile-de-France Ile-de-France Paris Activity type Research Organisations Administrative Contact Virginie Chameroy (Mrs.) Links Contact the organisation Opens in new window Website Opens in new window EU contribution € 755 604,00 Participants (15) Sort alphabetically Sort by EU Contribution Expand all Collapse all CENTRE EUROPEEN DE RECHERCHE EN BIOLOGIE ET MEDECINE France EU contribution € 440 840,00 Address Rue laurent fries 1 67404 Illkirch graffenstaden See on map Region Grand Est Alsace Bas-Rhin Activity type Research Organisations Administrative Contact Steve Brooks (Dr.) Links Contact the organisation Opens in new window Website Opens in new window MARTIN-LUTHER-UNIVERSITAT HALLE-WITTENBERG Germany EU contribution € 229 800,00 Address Universitatsplatz 10 6108 Halle See on map Region Baden-Württemberg Stuttgart Stuttgart, Stadtkreis Activity type Higher or Secondary Education Establishments Administrative Contact Sigrid Köhne (Dr.) Links Contact the organisation Opens in new window Website Opens in new window UNIVERSIDADE FEDERAL DO RIO DE JANEIRO Brazil EU contribution € 285 474,00 Address Av brigadeiro trompowski sn 2 21941 590 Rio de janeiro See on map Activity type Higher or Secondary Education Establishments Administrative Contact Marcello Fantappie (Prof.) Links Contact the organisation Opens in new window UNIVERSIDADE DE SAO PAULO Brazil EU contribution € 411 665,00 Address Rua da reitoria 109 butanta 05508 900 Sao paulo sp See on map Activity type Higher or Secondary Education Establishments Administrative Contact Kem Yoshida (Mr.) Links Contact the organisation Opens in new window Website Opens in new window ALBERT-LUDWIGS-UNIVERSITAET FREIBURG Germany EU contribution € 374 400,00 Address Fahnenbergplatz 79098 Freiburg See on map Region Baden-Württemberg Freiburg Freiburg im Breisgau, Stadtkreis Activity type Higher or Secondary Education Establishments Administrative Contact Manfred Jung (Prof.) Links Contact the organisation Opens in new window Website Opens in new window FUNDACAO OSWALDO CRUZ Brazil EU contribution € 866 520,00 Address Avenida brasil 4365 21040 900 Rio de janeiro See on map Activity type Research Organisations Administrative Contact Maurício Zuma (Mr.) Links Contact the organisation Opens in new window Website Opens in new window INSERM TRANSFERT SA France EU contribution € 313 190,00 Address 10 rue d'oradour-sur-glane - parisante campus 75015 Paris See on map Region Ile-de-France Ile-de-France Paris Activity type Private for-profit entities (excluding Higher or Secondary Education Establishments) Administrative Contact Louis Jammayrac (Mr.) Links Contact the organisation Opens in new window Website Opens in new window KANCERA AB Sweden EU contribution € 952 100,00 Address Banvaktsvagen 22 karolinska institutet science park 171 48 Solna See on map Region Östra Sverige Stockholm Stockholms län Activity type Private for-profit entities (excluding Higher or Secondary Education Establishments) Administrative Contact Martin Norin (Dr.) Links Contact the organisation Opens in new window Website Opens in new window ADLEGO BIOMEDICAL AB Sweden EU contribution € 184 863,00 Address Box 42 751 03 Uppsala See on map Region Östra Sverige Östra Mellansverige Uppsala län Activity type Private for-profit entities (excluding Higher or Secondary Education Establishments) Administrative Contact Urban Höglund (Mr.) Links Contact the organisation Opens in new window Website Opens in new window GRIFFITH UNIVERSITY Australia EU contribution € 0,00 Address Kessels road nathan 4111 Brisbane See on map Activity type Higher or Secondary Education Establishments Administrative Contact Nicki Church (Mrs.) Links Contact the organisation Opens in new window Website Opens in new window THE UNIVERSITY OF QUEENSLAND Australia EU contribution € 0,00 Address St lucia 4072 Brisbane See on map Activity type Higher or Secondary Education Establishments Administrative Contact Lyn Fairlie (Mrs.) Links Contact the organisation Opens in new window Website Opens in new window UNIVERSITA DEGLI STUDI DI ROMA LA SAPIENZA Italy EU contribution € 284 016,00 Address Piazzale aldo moro 5 00185 Roma See on map Region Centro (IT) Lazio Roma Activity type Higher or Secondary Education Establishments Administrative Contact Cinzia Murdocca (Mrs.) Links Contact the organisation Opens in new window Website Opens in new window UNIVERSITY OF EAST ANGLIA United Kingdom EU contribution € 334 241,00 Address Earlham road NR4 7TJ Norwich See on map Region East of England East Anglia Norwich and East Norfolk Activity type Higher or Secondary Education Establishments Administrative Contact Yvonne Kirkham (Mrs.) Links Contact the organisation Opens in new window Website Opens in new window Universidade Federal de Viçosa Brazil EU contribution € 268 680,00 Address Av. p.h. rolfs s/n 36570-000 Viçosa See on map Activity type Higher or Secondary Education Establishments Administrative Contact Daniel Marçal De Queiroz (Mr.) Links Contact the organisation Opens in new window Website Opens in new window INSTITUT PASTEUR France EU contribution € 298 598,00 Address Rue du docteur roux 25-28 75724 Paris See on map Region Ile-de-France Ile-de-France Paris Activity type Research Organisations Administrative Contact Marie-Laure Rosso (Dr.) Links Contact the organisation Opens in new window Website Opens in new window
