Scientific Literature Banner

[Abstract] Integrated Drug Discovery Engine for the Development of the Next-Generation Kinase Inhibitors

Through a combination of scientific and technological platforms oncodesign as developed a drug discovery engine allowing the fast development of new drugs candidates.  Using our technologies and capabilities: Medicinal chemistry, in vitro and in vivo Pharmacology, Phenotypic screen, Pharmaco-imaging and DMPK, we contribute to the development of new drugs on a service, partnership or licensing basis. Our medicinal chemistry technology Nanocyclix, is based on the macrocyclization of small Lead-like molecules and is the core of our drug discovery programs. It is a kinase-focused library of small macrocycles, designed in a chemocentric approach to identify attractive and selective kinases inhibitor across the kinome. All the compounds are in the drug-like properties space and hit compounds display nM potencies and good selectivity against a small number of kinases.  Nanocyclix design relies on the macrocyclization paradigm of known hinge binder scaffolds resulting in tighter binding site recognition, potency and selectivity towards the ATP site. Examples of H2L and LO will be presented to illustrate the value of the Nanocyclix approach in several indications ranging from Oncology to Immuno-inflammation and Parkinson disease.

Alexis Denis's Biography

Dr. Alexis, Director Discovery Medicinal Chemistry has been working in the R&D of pharmaceutical companies for 30 years (Aventis, Pfizer, Mutabilis, GSK, OncoDesign). His expertise covers all the aspects of Drug Discovery, Lead generation and optimization, structural based drug design approaches (successfully applied to several kinases and proteases), prodrugs, boron based medicinal chemistry, DMPK in several therapeutic areas : oncology, anti-infective, inflammatory and metabolic diseases. During his career, he contributed to the development of several drug and clinical candidates going to Phase I and beyond including a marketed antibacterial. He is the co-author of 35 patents and more than 30 research papers.