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Small molecules for biological targets

Objectives

Our team designs, synthesizes and evaluates small molecules inhibitors or modulators of biological targets. Our methodology is based on a rational approach, including molecular dynamics, virtual screening, medicinal chemistry, biophysical technics (NMR, TSA…) and structural biology. We use theses small molecules as tools to explore the biological pathways involved in cancer and/or open the route to novel therapeutics.

Projects

1.       The voltage-dependent anion channel VDAC-1

VDAC-1 is a channel located in the outer membrane of mitochondrial, whose function is crucial for cell survival and energy metabolic pathways. VDAc-1 is also involved in apoptosis and mays play a role in metastasis formation. To better assess the role of VDAC in cancer celles, and possibly validate the pharmacological targeting of the associated pathways, we seek to develop specific VDAC ligands capable of modulating its activity.

2.       Design of molecules modulating the CK2 kinase activity for therapeutic purposes

CK2 is a protein kinase involved in numerous pathologies, notably in cancer and viral infections. The structural particularity of CK2 is to exist in cells in two constitutively active forms (CK2α and CK2α2β2). To better understand the function of CK2 and the respective role of CK2α and CK2α2β2, we are developing specific CK2 inhibitors targeting allosteric sites.

Other projects include :
–    the design of ABCG2 inhibitors (Collaboration P. Falson, Lyon).
–    the development of NMR-based approaches for fragment-screening against GPCR (ANR NanoWAC, Prof C. Demesmay, ISA, University Lyon1).

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Publications