The 31st Camerino-Cyprus-Noordwijkerhout Symposia (May 19–23, 2013, in Camerino, Italy) are a series of international conferences on the medicinal chemistry, biology, and pharmacology of cellular receptors.
Receptors are proteins that capture biological messages given by a variety of bioactive chemicals, including neurotransmitters and hormones, and transform them into signals that alter the biology of cells. Notably, receptor signaling can be ad hoc modulated by exogenous molecules that either stimulate the receptors or block their stimulation. Hence, receptors offer great opportunities for pharmacological intervention and are the most common drug targets.
Professor Stefano Costanzi of American University is a member of the scientific committee of the 31st Camerino-Cyprus-Noordwijkerhout Symposium and will cochair a one-day session entitled “Structure-Based Discovery of Ligands of G Protein-Coupled Receptors: Finally a Reality.”
Generally speaking, experimentally determined three-dimensional structures of drug targets are invaluable tools for the rational design of drugs. For G protein-coupled receptors (GPCRs), a large family of integral membrane proteins that mediate a vast array of physiological
functions and are widely targeted by pharmaceutical agents, experimental structural studies have been historically very challenging. However, due to a number of scientific and technical
breakthroughs such studies recently became possible and entered a phase of rapid expansion that brought about the solution of the structures of many of the members of the GPCR family.
Notably, the 2012 Nobel Prize in chemistry was awarded to Robert Lefkowitz and Brian Kobilka, two researchers who have devoted their careers to unraveling the structure and the functioning of these receptor proteins.
The session cochaired by Costanzi will focus on the impact that these breakthroughs are having on the computer-aided, structure-based discovery of novel modulators of GPCRs. Specifically, a panel of two cochairs and eight speakers from academia, industry, and government agencies will discuss how these advancements are providing an increasingly more solid platform for the discovery and design of novel GPCR modulators. Moreover, they will discuss the possibility of employing experimentally solved GPCR structures as templates for the construction of models of other members of the GPCR family, a field in which Prof. Costanzi specializes. State-of-the-art, current challenges and future directions will be discussed. Moreover, as a follow-up to the session, a thematic issue edited by Costanzi will be published in the journal In Silico Pharmacology.
Prof. Costanzi has been actively conducting research on the rational discovery of GPCR modulators for many years. A graduate of the University of Camerino, where he started his research on GPCRs as a PhD student and, subsequently, a postdoctoral fellow, he recently joined American University after 10 years as a researcher at the National Institutes of Health. At AU, with a team of undergraduate and graduate students, Costanzi has established a strong research program on molecular and computational pharmacology of GPCRs, mainly focused on the identification of modulators of receptors found in the central nervous system.