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Course Proposal for ULLA Summer School 2015 Course title (short and descriptive): Medicinal chemistry for drug discovery and for understanding biological processes Course leader: Name: Pr. Sandrine Ongeri Organisation: Faculty of Pharmacy, University of Paris Sud, CHATENAY-MALABRY, France e-mail: [email protected] Teaching staff : Dr. Abdallah Hamze (Univ Paris Sud), Pr. Tap Ha-Duong (Univ Paris Sud), Dr. Serge Mignani (Sanofi-Aventis - Head Medicinal Chemistry; Consultant for Pharmaceutical industries and Institutes, USA, France, India, Morroco … ) Duration of course: [ X ] one day (max 6 hrs)* [ ] two days (max 12 hrs) Course level: [x] basic Prior knowledge required (if any): [ ] advanced Course description (max. 1/2 page or 300 words): Medicinal Chemistry: Drug Sources (1h30, Dr. A. Hamze) Design, identification and preparation of biologically active compounds, the study of their metabolism, the interpretation of their mode of action and the construction of structureactivity relationships (SARs): examples of drug discovery and information on the drug discovery process. Sources of drug discovery from natural and synthetic molecules; Interactive problems in Medicinal Chemistry by using WIMS WWW Interactive Multipurpose Server (different classes of drugs will be studied: Asthma, Cancer, Hypertension...) Principles in Biomolecular Modeling and in silico Drug Design (1h30, Pr. T. HaDuong) This lecture will present the principles and the applications of the main molecular modeling tools used in the structure-based drug design field: Modeling of the proteins 3D structures and dynamics; Molecular docking; Virtual screening; Protein-protein interactions. Chemicals tools to understand biological processes (1h30, Pr. S. Ongeri) Characterization of protein-protein and ligand-protein interactions in particular by Label-free ligand binding assays (SPR, ITC, TDA, RMN…) and labeled-ligand binding assays (with fluorescent, radioligand and fluorinated ligand) From small-molecules to bioconjugates via nanoparticles as new anticancer agents: feasibility, challenges and opportunities (1h30, Dr. S. Mignani)