Medicinal Chemistry in Academia – New Small Molecule Modulators for the Chemical Biology Toolbox
Marc Nazare,
Group Leader Medicinal Chemistry,
Leibniz-Institut für Molekulare Pharmakologie FMP, Berlin
The Chemical Biology platform at the Leibniz-Institut fuer Molekulare Pharmakologie (FMP) provides integrated access to HTS and Medicinal Chemistry hit-to-chemical tool development for academic projects on a collaborative basis. In three case studies, the approach and workflow for the identification of new tools will be illustrated. The first study will highlight the successful identification of selective MALT1 paracaspase inhibitors for the treatment of diffuse large B-cell lymphoma, which were derived from antipsychotic drugs by a screening approach. The second study will describe the hit identification, successful rescaffolding and chemical optimization towards drug-like, cellular active inhibitors of the phosphatase SHP2. These inhibitors may have the potential to attenuate tumor metastasis as well as intrinsic and acquired resistance to BRAF targeted cancer drugs. Finally, the third investigation will describe the development of an active cartilage targeting imaging probe for the in-vivo visualization of cartilage lesions.
|
|
