Accueil > Événements > Séminaires

Séminaire IBMM

Venoms to drugs

Prof. Paul F. Alewood (Division of Chemistry and Structural Biology, Institute for Molecular Bioscience, University of Queensland, Brisbane, Australia)

publié le , mis à jour le

Le Mardi 02 Octobre 2012 à 14h
UM1 Faculté de Pharmacie, amphithéâtre D

Many plant and animal families have developed distinctive chemical strategies for interacting with other organisms in their environment. As such they have provided a reservoir of bioactive chemicals that represent major sources of lead compounds for drug development.

The Conidae are a group of venomous marine gastropods (cone snails) that are found in tropical and sub-tropical waters. Venoms contained in the venom ducts of Conus species are delivered by a harpoon to rapidly immobilise prey. Most venoms so far examined have yielded an array of low molecular weight microproteins, the conotoxins, which typically contain cysteine rich polypeptide chains of 10–30 amino acids and are highly constrained by two to four disulfide bridges. Of particular interest is the high stability, potency and extreme selectivity of different conotoxins for ion channel receptors which include sodium, potassium and calcium receptors, the NMDA receptor and nicotinic acetylcholine receptors plus more recent molecules that target the noradrenaline transporter and G-coupled protein receptors.

In a program designed to exploit the potential of Australian Conus species we have isolated, characterised and chemically synthesised a broad range of novel conotoxins. Subsequently, we have determined their three dimensional structures and in many cases their pharmacology. In general the conotoxins have well-defined tertiary structures with many elements of protein secondary structure present. Furthermore, their frameworks have considerable rigidity that allow precise structure activity relationships to be developed. This has led to two clinical candidates (Xen2174 and AM336) from our laboratories that target chronic pain.

Contact local IBMM : Dr. Jean-Alain Fehrentz (DAPP)


Ajouter un événement iCal