Madrid Second Summer School
The second edition of the SEQT Summer School on “Medicinal Chemistry in Drug Discovery: The Pharma Perspective” has become a major success. It took place in San Lorenzo de El Escorial (Madrid, Spain) on 26-29 June, 2011. This second edition of the Summer School, an event sponsored by the European Federation of Medicinal Chemistry (EFMC), was organized by the Spanish Society of Medicinal Chemistry (SEQT) and Janssen with the aim of approaching the pharma industry to young researchers, both graduate students and post-doctoral associates working in the chemistry and health sciences related fields.
During the three days of the school, 65 participants coming from seven different countries around the world gathered together in the first-class facilities of Euroforum-Felipe II. The attendants (30% of whom were from the industry and the remaining 70% came from academia) had the opportunity to learn about the latest research trends in pharmaceutical drug discovery and development illustrated through real case studies led by an exceptional panel of industry experts currently working at international pharma industries.
The School started on with the opening session led by Prof. María L. López-Rodríguez (SEQT President), Dr. Javier Fernández-Gadea (Director of Basic Research at Janssen Spain) and Prof. Gabriele Costantino (EC member, representing EFMC). Then, during three intense days, an enthusiastic teaching team, composed by Kristof van Emelen (Janssen), Mark Bunnage (Pfizer), Jordi Gràcia (Almirall), Víctor Rubio (Faes Farma), Rob Young (GlaxoSmithKline) and José Cid (Janssen) handled different case studies in a very interactive manner fostering the discussion among the participants, organized during all the school in several work-teams. The sessions covered a number of topics dealing with the different stages of modern research and development in industry. Among them, the speakers considered essential aspects about target selection and hit design and development, with a special emphasis on the pharmacokinetic properties. Also, the importance of the scale-up and production processes was also highlighted.
The participants rated both the teachers and the information they provided very high (an average of 4.65 out of 5.00). The open interactive atmosphere was deeply appreciated. The inclusion of questions during the cases studies as well as sessions with questions and problems based on the preceding talks was extremely successful. In addition to the case studies, two poster sessions gave the opportunity to the attendants to present their works and to discuss with the teachers and the senior participants the most significant aspects of their research. In addition, the teachers together with the organizing and scientific committee selected 15 posters to be presented as short oral communications by the young researchers. These sessions were also highly valued by the participants.
The venue, conveniently located close to Madrid (in the pleasant village of San Lorenzo de El Escorial), was Euroforum Felipe II. The place was originally built as a luxury hotel and situated in a privileged residential area, among the forest and half-way up the Abantos massif. Today it has been turned into the modern and comfortable Executive Development Centre.
All in sum, the motivating scientific environment during the sessions and the friendly and informal atmosphere, together with the careful organization and the availability of the teachers throughout the school, were highly appreciated by the participants who praised the school as highly productive, interesting and formative event.
María Luz López Rodríguez
Silvia Ortega Gutiérrez
Javier Fernández Gadea
The XXXI Edition of the European School of Medicinal Chemistry has Successfully been Held in Urbino (Italy)
The XXXI edition of the European School of Medicinal Chemistry (ESMEC) has been held as usual in the Renaissance scenario of Urbino from July 3 to July 8, 2011. Of a total of 160 participants who have attended the this years edition, more than 65 % was constituted by PhD, master of post-doctorate students, 20 % by researchers from the academia and 15 % by researchers from industry. Although the participation to the School is a requirement for many Italian doctorate programs in medicinal chemistry, and thus the majority of the registrants came from Italy, the about 20 % of non Italian participants is an indication of the growing interest that the School is gaining around Europe. Interest that this year was particularly pushed by the appealing scientific program, by the quality of the invited speakers, and by some fellowships offered by the School, by EFMC, and by Farmindustria. In line with the well established format based on a four daily sessions, this year the School has covered the following topics: Infectious Diseases: Bacterial and Mycobacterial Infections. The Problem of Bacterial Resistance; Protein-Protein Interactions in Drug Discovery; Organo- and Bio-Catalysis in the Synthesis of Bioactive Compounds; Hot Topics.
The first session on Bacterial and Mycobacterial Infections has seen Alan Kozikowski (University of Illinois, USA) and Gian Maria Rossolini (University of Siena, I) introducing the misuse of antibiotics and the rise of bacterial resistance as a major driver of unmet clinical needs. In fact, despite the successes of the antibacterial chemotherapy, resistance to several antibiotic classes began to emerge in Gram-positive bacteria in the United States during the 1990s. The emergence of multidrug-resistant strains of S. pneumoniae, Enterococcus faecium, and S. aureus emphasizes the critical need to develop novel antibiotics to treat serious Gram-positive infections. In the second half of the session, Sergio Lociuro (THOT consulting Sagl, Maroggia, CH) has focused on new approaches to fight against bacterial resistance like optimising “old” classes, searching new classes acting on “old” targets, searching new classes acting on never exploited targets, preferring broad spectrum agents vs. narrow spectrum vs. single pathogen agents. Furthermore, Alan Kozikowski, with a second lecture on this topic, has illustrated the use of high throughput screening (HTS), medicinal chemistry, and cell biology in the discovery of new drugs against resistant strains of TB.
The second session was devoted to Protein-Protein Interactions (PPIs) in Drug Discovery and provided participants with an up-to-date overview of fundamental concepts and strategies, as well as biophysical and computational approaches and tools in a field of paramount importance. The first speaker, Kumlesh Dev (Trinity College Dublin, IR), focused his talk on the new concept of generating compounds that alter receptor function from the inside (i) of the cell by regulating intracellular (i) trafficking; in other words, on the discovery of i‐agonists and i‐antagonists, where the “i” refers to inside and intracellular regulation. The second speaker, Domenico Raimondo (University “La Sapienza”, Roma, I), presented computational approaches for studying protein-protein interactions such as protein modeling, genome functional annotation, protein structure analysis and characterization of protein-protein and protein-DNA complexes. The last two lectures given by Alessandro Padova (Siena Biotech, I) and Kristian Strømgraard (University of Copenhagen, DK) have focused the possibility of modulating protein-protein interactions to find new therapies for cancer and neurological disorders or chronic neurodegenerative diseases.
The third session on Organo- and Bio-Catalysis in the Synthesis of Bioactive Compounds has seen the presentation of very interesting approaches and methodologies in organic synthesis directed to potential drug molecules. Paolo Melchiorre (Institute of Chemical Research of Catalonia, Tarragona, E) in the opening lecture has addressed the emerging field of aminocatalytic cascade reactions that recently proved to be a new strategy to recreate the intricate structural scaffold and related complex stereochemistry of natural-like compounds with very high fidelity. The second talk, given by Marco Bella (University “La Sapienza”, Roma, I) was strictly connected to the previous one since it has given an overview of the asymmetric organocatalysts which act without the formation of any covalent bond to the substrate. The third lecture, by Marco Bandini (University of Bologna, I), has illustrated the advantages of the synthesis of complex molecules provided by a combination of the organo- with organometallo-catalysis. The last two lectures have been dedicated to biocatalysis. Kurt Faber (University of Graz (A) has presented the application of ene-reductase-mediated asymmetric synthesis to the preparation of several different bioactive compounds, whereas Roland Wohlgemuth (Sigma-Aldrich, Buchs, CH) ha given an overview of biocatalytic transformations in the context of the growing importance of metabolites as drugs, drug-derived products, analytical standards, tools for elucidating biochemical pathways and for metabolomic studies.
The last day has covered some hot topics. More in detail, recent progresses in the structure and function of ion channels, transporters and G-protein coupled receptors have been illustrated by Chris Ulens (Laboratory of Structural Neurobiology, Leuven, B) who showed how the several three-dimensional structures of GPCR, ion channels and transporter now available may help the design of specific modulators. Olivier Bezencons (Actelion Pharmaceuticals Ltd, Allschwil, CH), starting from Aliskiren, the first Direct Renin Inhibitor (DRI) clinically available, presented the discovery of a new class of DRI with a piperidine-based structure; one of these compounds, ACT-077825 is presently in clinical trials for the treatment of hypertension. Henk Stunnenberg (Radboud University, Nijmegen, NL) showed how the systems biology approach, which considers the cell as a system whose components interact in a certain way in normal conditions or in response to a chemical or genetic perturbation, can be applied to find treatments for leukemia. The last speaker of this edition was Nicola Curtin (University of Newcastle upon Tyne, UK). She focused her talk on poly(ADP-ribose) polymerases (PARPs) that are enzymes activated by DNA strand breaks and involved in DNA repair and on the application of PARP inhibitors in cancer therapy. In fact they are one of the first classes of compounds that interact in a synthetic lethal manner with mutations in the genes encoding proteins involved in DNA repair. Some PARP inhibitors, are now in clinical trials for BRCA1 or BRCA2 mutants tumors, for triple-negative breast cancer, ovarian cancer and other solid tumors.
The didactic program of the School was completed by two workshops on protein-protein interactions in drug discovery and on organo- and bio-catalysis in the synthesis of bioactive compounds, promoting a closer interaction between students and lecturers and among students with different background and know-how. Furthermore, the PhD students following the last year of PhD course and them coming from foreign countries have been invited to present a poster on their research during two poster sessions, where results and methodologies have been freely discussed and the 10 best posters have been selected for an oral presentation.
A very interesting part of the School was a round-table organized by Farmindustria, the Italian association of pharma industries, to discuss on ‘Medicines and Public Private Partnerships: From Labs to Patients’. The meeting has seen a large and active participation of young researchers and PhD students.
As confirmed by the analysis of the evaluation questionnaires completed by participants, the School has certainly achieved its scientific and didactic aims, thus confirming the success of a format that nicely mixes up advanced seminars and didactic introductions and workshops. The informal environment and the appealing social program have also contributed to promote a productive interchange between participants. In conclusion, the Scientific Committee hope that ESMEC-Urbino school could contribute to keep at a very high level the didactic offer of the EFMC. With the hope to continue along this way, the organizers are looking forward to seeing you in Urbino for the XXXII edition, in July 2012.
Univ. of Parma, IT
Gazi Univ., TR
Lucija Peterlin Masic
Univ. of Ljubljana, SI
Univ. of Geneve, CH
Univ. Halle-Wittenberg, DE
Pfizer, Sandwich, UK
Gerhard F. Ecker President
Roberto Pellicciari Past Pres.
Koen Augustyns Secretary
Rasmus P. Clausen Treasurer
Javier Fernandez Member
Mark Bunnage Member
Peter Matuys Member