Design de complexes multitâches pour la thérapie du cancer et leur libération thermosensible ciblée


Annie Castonguay

Institut national de la recherche scientifique


Domaine : cancer

Programme chercheurs-boursiers - Junior 1

Concours 2015-2016

The increasing costs of healthcare hamper the capacity of healthcare providers to effectively treat disease, thus providing impetus for developing less expensive, more effective medicine. The greatest challenge of modern drug discovery does not only lie in finding compounds that display a high therapeutic activity, but also in optimizing drug candidates' affinity and selectivity toward certain biological targets.

The overall objective of this multidisciplinary program is to create novel treatment modalities with improved safety margin (increased therapeutic effect combined to lower side effects), using cancer as a model, a disease that is devastating the lives of countless Quebecers. Targeted drug delivery is a covoted method to overcome the affinity and the selectivity barrier for molecules with a high therapeutic value. It consists of delivering the medication to a patient in a manner that increases the local drug concentration in some parts of the  body relative to others; the therapeutic agent is then part of a shuttle, and is carried to a specific target in proximity to the diseased tissue before being released. Multitasking organometallic therapeutics (MOTs) are a new class of drugs with superior activity, able to promote cell death by simultaneously targeting selected signal transduction molecules, leading to additive/synergistic therapeutic effects. By combining the unique targeting capabilities of aptamers with the cancer-killing ability of ruthenium-based "MOTs", it will be possible to create novel powerful tools to overcome the numerous problems associated with existing chemotherapies. This union will allow sensitive discrimination between healthy and diseased tissue. In other words, in contrast to traditional chemotherapeutic agents, carefully engineered ruthenium hybrids will target and attack the cancer cell so that healthy cells are less severely affected.