Organization: 

Institut Pasteur Lille

First Name: 

Nicolas

Last Name: 

Willand

Country: 

France

E-mail: 

nicolas.willand@univ-lille2.fr

Phone: 

+33664289100

Statement: 

The challenges of the TB-drug boosters development are addressed by a consortium of highly complementary partners working in the field of tuberculosis (Priscille Brodin and Alain Baulard teams at Pasteur Institute, Lille, France) and medicinal chemistry (Benoit Déprez and Nicolas Willand team at Pasteur Institute, Lille, France). The combined efforts of our research consortium led to the design and development of first compounds able to inhibit a transcriptional regulator EthR, known to down regulate ethionamide’s bioactivation. Our results published in Nature Medicine (2009), ACS Chemical Biology (2010) and J.Med.Chem. (2011) demonstrated that the sensitivity of M. tuberculosis to ETH can be substantially increased in vitro and in vivo using specific EthR inhibitors. Critically, our booster compounds were able to triple the activity of ETH in a TB-infected mice model. We are currently working on the development of a preclinical candidate. In parallel, we are identifying new chemotypes, which will display different risk profiles, using HTS or Fragment-based drug design strategies. Therefore, I will definitely enjoy being member of the working group on new drugs to share scientific work with all members.

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