The research activities of the Medicinal & Phytopharmaceutical Chemistry team are divided into two themes:
1) Medicinal Chemistry: Our drug discovery strategies encompass both a target based as well as a phenotypic approach. i) Target-based approaches focused on the design of metalloenzyme inhibitors with particular emphasis on inhibiting the M1(alanyl) and M17(leucyl) aminopeptidase families. Aminopeptidases are involved in many metabolic disorders (angiogenesis, inflammation, autoimmune diseases, and cognitive decline) and are essential for the development of pathogenic agents (Plasmodium, Toxoplasma, Neisseria). We have discovered a modular platform, based on aminobenzosuberone scaffold, inhibiting potently and selectively each aminopeptidase family. Several medicinal chemistry programs (recombinant enzymes, SAR studies, prodrugs) are currently in progress. ii) Phenotypic approach against Plasmodium falciparum to identify novel fast acting, transmission blocking anti-malarial agents as well as exploration of their mode of action.
2) Phytopharmaceutical activities: Our plant protection activities are focalized on grapevine trunk diseases, which have disastrous consequences for vine yield and longevity. No treatment are currently available, thus we developed different strategies to address these issues: i) mode of action investigation on known fungicides, ii) new specific fungal target identification, iii) plant-pathogen interactions analysis and iv) resistance study of Vitis Vinifera subspecies.
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Team Leader – Assistant professor