The main focus of our research is the design and synthesis of inhibitors and related synthetic tools for the study of Zn-proteases, the most densely populated class of proteolytic enzymes in human. Since they play central role in multiple biological functions and are often involved in several pathological conditions (such as cancer, neurodegenerative disorders, inflammatory and cardiovascular diseases), the discovery of small-molecules able to target efficiently and selectively these enzymes is of paramount importance for various biochemical and medicinal applications (pharmaceutical agents, diagnostic tools e.t.c.). To address this intriguing challenge, we have selected phosphinic peptides, a class of privileged organic compounds that present unique properties among other types of inhibitors described in the literature.
Over the past years we have been involved in projects concerning the discovery of potent and selective inhibitors of Zn-proteases. Fruitful collaborative work with leading biochemists in the field (MMPs, vasopeptidases: Dr Laurent Devel, ER aminopeptidases: Dr Efstratios Stratikos) and extensive SAR studies have led in several cases to the discovery of inhibitors with unique properties such as of the following (read more by hovering over each structure):
Another area of interest to our group is natural products synthesis. We seek for the development of new methodologies triggered by the challenges that the complexity of these molecules imposes. Check out the development of a novel Lewis-acid catalysed self-assembled Diels-Alder reaction which enabled the synthesis of Abyssomicin C core structure:
created with
Website Builder Software .
