[EN] Make it cyclic: A paradigm for the discovery of selective kinases inhibitors “Nanocyclix”

Alexis Denis, Directeur Activités Découverte
23 mai 2019 – 17h

Cyclization in drug discovery is a growing paradigm that recently yielded registered drugs. Oncodesign has developed an Integrated Drug Discovery platform Nanocyclix to synthesize small libraries of macrocycles and design specific molecules through fragment and structural based drug design to identify attractive and selective kinases inhibitor.
Nanocyclix molecule are in the drug-like space and display nM potencies and good selectivity across the kinome. Nanocyclix design is based on the macrocyclization paradigm of known hinge binder scaffolds or small fragments resulting in lower of entropic penalty.
The resulting tighter binding site recognition, increases potency and selectivity towards the ATP site.
Key learnings and strength of the Nanocyclix paradigm will be exemplified by the development of a clinical PET tracer and Lead to candidate programs in Oncology, Parkinson Disease and Immuno-inflammation.

Key Learning objectives

  • Integrated Drug Discovery.
  • Medicinal Chemistry technology Nanocyclix based on macrocyclization of small Lead-like molecules and fragments.
  • Kinase-focused library designed to identify attractive and selective kinases inhibitor.
  • Macrocyclization paradigm of known hinge binder scaffolds resulting in tighter binding site recognition, potency and selectivity towards the ATP site.
  • Examples of Nanocyclix in several indications ranging from Oncology to Immuno-inflammation, and PET Imaging.

About our speaker Alexis Denis

Dr. Alexis Denis, 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 and fragment (successfully applied to several kinases and proteases), boron based medicinal chemistry in several therapeutic areas: oncology, anti-infective, inflammatory and metabolic diseases. During his career, he contributed to the development of several drug 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.

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