Pascal Dao Email & Phone Number

Paris, Fr

The initial results obtained during my postdoc led to the creation of YUKIN Therapeutics in 2018where I worked as Senior Scientist in lead optimisation. Based on my medicinal chemistrybackground, I have overviewed the drug discovery process with the management of a PhDStudent (Cifre fellowhip) and a CROs for the lead optimisation and scaffold hopping. Thescreening cascade I implemented allowed the identification of the lead compounds and a deepunderstanding of the SAR. The PK of selected compounds and the optimisation of formulations Isupervised led to in vivo efficacies studies in collaboration with the biologists of the team.

I worked on the development of new NIK inhibitors to potentiate current immunotherapytreatments in cancer. Starting from the first set of compounds, I was able to develop a new setof compounds with high diversity for SAR evaluation and scaffold diversity with a multiparametricoptimization strategies. This includes the design/optimization of new synthesis routes and theirimplementation at the bench to obtain the highest diversity of compounds possible from simpleto complex compounds with the capacity to use a large variety of chemicals reactions. With thisnew set of more than 100 compounds, I have a develop a full phenotypic screening for thecharacterization of their potency to restore a senescence program with the activation of theimmune system in the tumour microenvironment devoid of toxicity on healthy or cancer cells. Afterthe target ID and characterisation of the mechanism of action, in collaboration with the biologistsI have setup the first in vivo efficacy studies.With this promising results in hand, we have developed a first collaboration leading to thecreation of YUKIN therapeutics.

As part of the development of a new laboratory, Prof Bernard Meunier has given the task ofdeveloping new research on the development of new diagnostic tools for the implementation ofnon-invasive tests by the design of new fluorescent probes for the early detection of amyloidplaques in the retina.I designed, synthesized and evaluated the new fluorescent probes for the early detection ofamyloid plaques in the retina. I was able to develop new synthetic way to obtain a variety ofbenzothiazole-based push-pull fluorophores. I determined their full photochemical propertiesand assessed there in vitro and in vivo properties.

Evaluation of the therapeutic combination of FAK and TRAIL inhibitors

Synthesis and biological studies of inhibitors of focal adhesion protein (FAK) with antiangiogenic and anti-tumor activityMy thesis work focused on rational design of new inhibitors of the focal adhesion protein (FAK)for the development of new targeted anti angiogenic and anti-tumor therapies. I participatedin the design, synthesis, purification and characterization of new molecules by multistep synthesis.As part of the development of new molecules, I have designed and optimized a new synthetic,high yield route to obtain the targeted compound using organocatalysis and microwave-assistedchemistry. I have setup and optimized the process for the evaluation of their inhibitory activityon purified protein (TR-FRET assays) for the characterisation of their kinase inhibitory activity. Ihave subsequently evaluated the anti-angiogenic and anti-tumour activity on several tumour celllines as well as the characterisations of mode of action (MoA) by ELISA, WB and microscopy

Hdr - Habilitation À Diriger Des Recherches

Education record

Doctor Of Philosophy - Phd, Medicinal And Pharmaceutical Chemistry

Master Of Science - Ms, Chemistry & Therapeutics

Bachelor Of Science - Bs, Biochemistry And Molecular Biology