Scientific Publication Macrocyclisation process

Nanokinib: a cyclic library of hinge binder.
A chemocentric approach for the discovery of selective kinases inhibitor

Nicolas GEORGE, Pascal ENDERITTER, Petra BLOM, Marie-Hélène FOUCHET, Alexis DENIS
& Jan HOFLACK

Oncodesign
Hearquarters: 20, rue Jean Mazen, B.P. 27627, 21076 Dijon Cedex, FranceFrançois Hyafil Research center: 27, avenue du Québec 91140 Villebon-sur-Yvette, France

Nanokinib, is a kinase focused library of small macrocyclic hinge binder, 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. Nanokinib design is based on the macrocyclisation paradigm of known hinge binder scaffolds resulting in tighter binding site recognition, potency and selectivity towards the ATP site. Exploring different lengths and functionalities of the cyclic linker allow populating the conformational space of every template and to identify an optimal match between the size and mobility of the binding site and the macrocyclic ligand. Potent and selective inhibitors of therapeutic kinases such as LRRK2, RIPK2 and ALK1 have been identified by this approach and their optimization to advanced lead will be briefly described.

nanokinib acs oncodesign

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