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Camerino, May 16-20,
2010
Trekking through
Receptor Chemistry
Program
Sunday, May 16th, 2010
Welcome
18:45 - M. Giannella (University of Camerino, I)
Opening lecture
19:00 - U. Hacksell (ACADIA Pharmaceuticals San Diego, USA) Discovery and
development of drugs for CNS diseases
20:30 - Welcome dinner
*******
Monday (morning), May 17th, 2010
9:00-9:10 - Starting on the right foot: selection criteria in lead discovery
(Chairman R. Thomas, I)
9:10-9:40 - R. E. Hubbard (University of York, Cambridge, UK) - Too much
choice: selecting which fragments to optimize
9:40-10:10 - E. H. Kerns (Wyeth Research, Princeton, USA) Integration of
drug-like properties in selection, optimization and biological assessment in
lead discovery
10:10-10:30 Coffee break
10:30-11:00 - C. Ghiron (Siena Biotech, Siena, I) The design, management and
maintenance of a screening collection
11:00-11:30 - P. Leeson (Astra Zeneca, SE) Can We Improve Compound
Quality?
12:30 Lunch
*******
Monday (afternoon), May 17th, 2010
15:00-15:10 New avenues to target G protein coupled receptors (Chairman R.
Leurs, NL)
15:10-15:40 M. Bouvier (University of Montreal, CA) Ligand-based GPCR
signalling; potential implications for drug discovery
15:40-16:10 G. Zaman (Schering-Plough Research Institute, NL) New avenues
to target 7-transmembrane receptors
16:10-16:30 Coffee break
16:30-17:00 M. Allegretti (R&D Dompι, I) Pharmacological characterization
of functionally selective CXCR inhibitors
17:00-17:30 M. Smit (LACDR, NL) Nanobodies as new GPCR modulators
17:30-18:00 S. Schann (Domain Therapeutics, F) mGluR4 positive allosteric
modulator: new paradigm for CNS indication treatment
18:00-18:30 R. Pellicciari (University of Perugia, I) Prospects for a
TGR5-mediated control of glucose homeostasis: focus on the clinical
candidate S-EMCA (INT-777)
19:30 Dinner
21:00 Social event
*******
Tuesday (morning), May 18th, 2010
9:00-9:10 - G protein coupled receptors: old landscape with new eyes
(Chairman D. Donati, I)
9:10-9:40 - G. Whitlock (Pfizer, UK) Design of BBB penetrant alpha1A
receptor partial agonists
9:40-10:10 - C. Enzensperger (University of Jena, D) The dopamine D1-family:
steps towards selectivity
10:10-10:30 - Coffee break
10:30-11:00 - A. Makriyannis (CY) The endocannabinoid proteins as drug
targets
11:00-11:30 - D. Piomelli (University of Irvine, USA) The endocannabinoid
system in the control of pain and emotion
11:30-12:00 - S. Ronzoni (NiKem Research, I) Novel potent and selective
ORL-1 antagonists with efficacy in animal models of Parkinson's disease and
neuropathic pain
12:00-12:30 P. S. Portoghese (University of Minnesota, USA) Relevance of
GPCR heteromers in the action of opioid analgesics
12:30 Lunch
*******
Tuesday (afternoon), May 18th, 2010
15:00-15:10 Applications of computational methods in lead discovery
15:10-15:40 M. S. Congreve (Heptares Therapeutics Ltd., UK) Stabilized
GPCRs for structure based drug design
15:40-16:10 K.-H. Baringhaus (Sanofi-Aventis, Detschland GmbH, D)
Computer-assisted lead finding of GPCR and ion channel modulators
16:10-16:30 Coffee break
16:30-16:40 Receptors and beyond (Chairman R.A. Glennon, USA)
16:40-17:10 P. J. L. Svenningsson (Karolinska University of Stockholm, SE
) Regulation of 5-HT receptors by p11
17:10-17:40 E. X. Albuquerque (Uiversity of Maryland, USA) Nicotinic
receptor function in the mammalian brain: modulatory properties and
influence of endogenous regulators
17:40-18:10 M. K. Schulte (University of Alaska Fairbanks, USA) Allosteric
modulation of neuronal nicotinic acetylcholine receptors
18:10-18:40 K. Mohr (University of Bonn, D) Dualsteric GPCR-targeting:
Fine-tuning binding selectivity and signalling pathway activation
19:30 Dinner
21:00 Social event
*******
Wednesday (morning), May 19th, 2010
9:00-9:10 - Polypharmacology: creating selective non-selectivity (Chairmen
C. Melchiorre / M.L. Bolognesi I)
9:10-9:40 - J. S. Mason (Lundbeck Research, DK) Polypharmacology: using it
to differentiate and as an advantage with selective non-selectivity
9:40-10:10 - R. Morphy (Schering-Plough, UK) Multi-target drug discovery -
past, present and future
10:10-10:30 - Coffee break
10:30-11:00 - C. J. Van der Schyf (NEOUCOM, USA) Multiple mechanism drugs
for neurodegenerative diseases and post-stroke neuroprotection
11:00-11:30 - M. B. H. Youdim (University of Haifa, IL) Multimodal
neurorestorative drugs acting at different brain regions and neuronal sites
for neurodegenerative disorders
12:30 Lunch
*******
Wednesday (afternoon), May 19th, 2010
15:00-15:10 Orexin antagonists as novel treatment of insomnia (Chairman H.
Timmerman, NL)
15:10-15:40 E. Ratti (GSK, I) Biology of the orexin system: focus on
sleep-related mechanisms
15:40-16:10 R. Di Fabio (GSK, I) Discovery of SB648868 as novel orexin
receptor antagonists for treatment of insomnia
16:10-16:30 Coffee break
16:30-17:00 A. J. Roecker (MERK & Co., USA) Discovery of potent diazepane-containing
dual orexin receptor antagonists for the treatment of insomnia
17:00-17:30 C. Boss (Actelion Pharmaceuticals, CH) Orexin receptor
antagonists - A new therapeutic principle in CNS disorders?
17:30-19:00 Poster session
19:30 Dinner
21:00 Social event
*******
Thursday (morning), May 20th, 2010
9:00-9:10 - Application of stem cell technology to drug discovery (Chairman
A. Makriyannis, USA)
9:10-9:40 - A. T. T. Chuang (GSK, USA) Application of stem cell technology
in drug discovery
9:40-10:10 - A. Bakker (Siena Biotech, I) Brain tumor stem cells as a tool
to identify novel therapeutics
10:10-10:30 - Coffee break
10:30-11:00 - R. Thomas (Siena Biotech, I) Successful modulation of tumor
stem cells with small molecule hedgehog pathway antagonists
11:00-11:30 - G. Gaviraghi (Siena Biotech, I) Therapeutic modulation of the
Wnt signalling pathway, an innovative approach for oncology and
neurodegeneration
11:30-12:00 Looking forward (M. Giannella - I, A. Makriyannis - CY, H.
Timmerman - NL)
12:00-12:30 D. J. Triggle (USA) The sustainability of pharmaceuticals in
the 21st century: the idle thoughts of an idle fellow
12:30 Lunch
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Thursday (afternoon), May 20th, 2010
15:00 Trip to Matelica and Visit to the Museo Archeologico and Museo
Piersanti; Visit to Lanciano Castle
21:00 Social dinner (Villa Fornari)
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