Program

Monday 16th 2016

Palazzo Ducale - Aula Arangio Ruiz

Session Title: "Modeling GPCRs in the Structural Biology Era"
Chairs: Stefano Costanzi (American University - USA)

Abstract

"Homology Modeling of a Class A GPCR in the Inactive Conformation: a Quantitative Analysis of the Correlation Between Model/Template Sequence Identity and Model Accuracy"
Stefano Costanzi
(American University - USA)

“Structural Insights into Transmembrane Receptor Signaling”
Andrew C. Kruse
(Harvard Medical School, Boston, MA - USA)

Coffee Break

"Revelations from GPCR Protein-Ligand Structures, with Key Roles for Water and the Prediction of Kinetics."
Jonathan S. Mason
(Heptares, Welwyn Garden City, UK)

"Structural Basis for G-Protein Selectivity Using Multiscale Dynamics and FRET Sensors"
Nagarajan Vaidehi
(City of Hope Duarte, CA, USA)

"Modelling the Cannabinoid 2 Receptor and Structure Based Studies of Agonist/Antagonist Molecular Switches"
Claudio Cavasotto
(IBioBA-CONICET-Partner Institute of the Max Planck Society, Buenos Aires, Argentina)

Lunch (Hotel "I Duchi")

Session Title: "Modeling GPCRs in the Structural Biology Era"
Chairs: Stefano Moro (University of Padua - Italy)

"Polypharmacology of Conformationally Rigid Nucleosides: Purine Receptors and Beyond”
Kenneth A. Jacobson
(NIDDK - NIH - Bethesda - USA)

"Molecular Modelling Studies on Adenosine Receptors and Their Ligands"
Diego Dal Ben
(University of Camerino - Italy)

"Mutant Muscarinic Receptors as Novel Chemogenetic Tools" 
Jurgen Wess
(NIDDK - NIH - Bethesda, MD, USA)

Abstract

Coffee Break

Conferment of "Laurea Honoris causa" to
Dr. Robert J. Lefkowitz

Palazzo Ducale - Aula della Muta
 

Vegan Dinner (Hotel "I Duchi")

Tuesday 17th 2016

Palazzo Ducale - Aula Arangio Ruiz

Session Title: "Understanding GPCR-Ligand Interactions"
Chair: Rob Leurs  (VU University Amsterdam, the Netherlands)

"Identification of Endogenous and Surrogate Ligands for Orphan G Protein-Coupled Receptors"
David E. Gloriam
(Univerisity of Copenhagen, Denmark)

"Structural Biology of the EDG Receptors"
 Mike A. Hanson
(GPCR consortium, USA)

Coffee Break

"GPCR Ligand Binding Kinetics: from X-Ray Structure to Understanding of  Antagonist Dissociation Kinetics"
Chris de Graaf
(VU University Amsterdam, the Netherlands)

"Fragment Llinking for GPCRs: a Case Study on Dopamine D3 Receptors"
Gyorgy M. Keseru
(Hungarian Academy of Science, Hungary)

"Revisiting Mechanism of Action and Clinical Profile of Choline Alphoscerate.
An Experience in the Field of Cognitive Dysfunctions"
Francesco Amenta
(University of Camerino, Italy)

Lunch (Hotel "I Duchi")

Session in memory of Dr. Wolfgang Froestl

Session Title: "Advanced Clinical Studies with Drugs for the Treatment of Alzheimer’s and Parkinson’s Disease"
Chair:  David A. Lowe (AC Immune SA - Switzerland)

"Tozadenant, a Potent and Selective Adenosine A_2A Receptor Antagonist "
Stephen I Bandak
(Biotie Therapies Inc. - USA)

"ANAVEX-2-73, a Sigma-1 Receptor Agonist"
Christopher U. Missling
(ANAVEX Life Science Corp. - USA)

"Azeliragon; A RAGE Antagonist in Phase 3 Clinical Trials for the Treatment of Alzheimer’s Disease"
Robert C. Andrews
(vTv Therapeutics - USA)

Tour to Tolentino: visit to "International Museum of Humor in Art"
and
Chapel of Saint Nicholas

Dinner and Music @ Area T - Tolentino

Wednesday 18th 2016

Palazzo Ducale - Aula Arangio Ruiz

Session Title: "Dopamine D₂-like Receptors: From Structure and Function to Potential Therapeutics"
Chair:  Amy H. Newman (NIDA-IRP, NIH - USA)

"D₂-Like Receptors as the Base of Multi-Target Directed Ligands for the Treatment of Schizophrenia"
Stefania Butini
(University of Siena - Italy)

"Novel Bitopic Ligands Based on the Sumanirole Pharmacophore Reveal Dopamine  D2 Receptor (D2R) Biased Agonism"
Alessandro Bonifazi
(NIDA-IRP, NIH- USA)

Coffee Break

"Implication of Multifunctional D3 Preferring Agonist as Therapeutic Agents in Parkinson’s Disease"
Aloke Dutta
(Wayne State University - USA)

"VK4-116 - A Novel and Highly Selective Dopamine D3 Receptor Antagonist That Attenuates Oxycodone and THC Self-Administration"
Amy H. Newman
(NIDA-IRP, NIH- USA)

Poster Session

Lunch (Hotel "I Duchi")

Session Title: "Beyond Receptor Chemistry: Transporters"
Chair: Richard A. Glennon  (Virginia Commonwealth University - USA)

"Transporters as Clinical Targets of Drugs: Amphetamines, New Psychoactive Substances and the Monoamine Transporter Cycle”
Harald H. Sitte
(Medical University Vienna - Austria)

"Direct Assessment of Conformational Changes Uncovers Functional
Regulation by K⁺ in a  Neurotransmitter: Sodium Symporter"
Claus Juul Løland
(University of Copenhagen - Denmark)

Coffee Break

"Beyond Monoamine Transporters: Organic Cation Transporters (OCTs)"
Malgorzata Dukat
(Virginia Commonwealth University - USA)

"Synthetic Cathinones: a New Class of Abused Substances and their Actions at Monoamine Transporters"
Richard A. Glennon
(Virginia Commonwealth University - USA)

"Remembering Maria Pigini and Her Two Decades of Imidazolines"
Fabio del Bello - Carla Ghelardini - Antonio Carrieri

Maria "Nelly" Pigini Awards

Dinner  (Hotel "I Duchi") & Musical entertainment by Filarmonici Camerti (Palazzo della Musica)

Thursday 19th 2016

Palazzo Ducale - Aula Arangio Ruiz

Session Title: "The Future"
Chair: David J. Triggle (SUNY University - USA)

"Publish and Perish: Where Is Scientific Publication Going?"
Chris R. Triggle
(Weill Cornell Medical College in Qatar - Qatar)

"Drug Discovery Innovation: The Evolving Role of Medicinal Chemistry"
Joel C. Barrish
(Achillion Pharmaceuticals, Inc. - USA)

Coffee Break

"What Can We Get from Natural Products and Alternative Medicine?"
Shyam S. Chatterjee
(Germany)

Abstract

"Zombies and Their Pharmacology. What Can Host-Parasite Relationships Teach us About New Pharmacological Approaches?"
David J. Triggle
(SUNY University - USA)

Abstract

11.30-12.00

"Summing Up"
Richard A. Glennon  (Virginia Commonwealth University - USA)

12.30

Social Tour to Ascoli Piceno and Social Dinner