Design and discovery of novel cathepsin S ligands and their evaluation as PET and fluorescent probes for oncology diagnosis

Organisation: Johannes-Gutenberg-Universität Mainz (JGU), Germany

Supervisors: Prof. Dr. Tanja Schirmeister and Dr. Christian Kersten

Hello readers! My name is Thales and I am a pharmacist with a passion for drug development, from discovery and design to delivery. I come from Belo Horizonte (BR), where I graduated from the Federal University of Minas Gerais with a degree in Pharmacy. Although I began doing phytochemistry research in my early years of study, my Pharmacy thesis concerned the combined virtual and experimental screening of a set known as Pathogen box against cruzain and rhodesain (TbCatL), two important parasitic cysteine proteases associated with neglected tropical diseases. I also studied Medicinal Chemistry for a year at Trinity College Dublin (IE), where I completed an internship in the synthesis of substituted porphyrins. After working for some time as a laboratory technician at my home university, I obtained my Erasmus Mundus Joint Master Degree in Nanomedicine for Drug Delivery from the Universities of Paris Cité (FR, the coordinating institution), Patras (GR), Angers (FR), and Pavia (IT). I wrote my master thesis on the development of cationic thermosensitive liposomal formulations at Thermosome GmbH in Munich (DE), where I continued afterward as a formulation scientist. While working on smart anticancer therapies, I grew interested in understanding how to harness the power of the immune system to fight disease. The cysteine protease cathepsin S is overexpressed in the tumor microenvironment, and its inhibition and silencing correlated with an increase in anticancer immunity. My role as DC5 of OncoProTools is to synthesize cathepsin S inhibitors and link them to reporters (i.e., fluorescent and radioactive labels). These conjugates could then be used as tools to study the tumor microenvironment and diagnose cancer. By combining different linkers and radionuclides, a theragnostic approach for these conjugates is also conceivable.