Small Molecule Synthesis and Medicinal Chemistry
Established in 2010 as the first medicinal chemistry lab of the University of Edinburgh campus at the Western General Hospital, the main goal of the Innovative Therapeutics Lab is the exploration and translation of novel chemical strategies to increase the efficacy and safety of cancer treatments.
This includes development of exquisitely selective inhibitors of kinases involved in cancer and novel prodrug strategies aimed at improving the clinical use of well-established chemotherapy drugs. The lab possesses a unique skillset within the Edinburgh Medical School, which covers small molecule synthesis, medicinal chemistry, prodrug design via bioorthogonal chemistry, polymer functionalization, peptide synthesis, in vitro screening, IP protection and technology commercialization. The lab has developed a portfolio of patented technologies and established a collaborative network -across and out with the University- of drug discovery experts from different specialties including cancer biologists, pharmacologists, clinical oncologists , entrepreneurs and venture capitalists, to promote the translation of such technologies.
Synthesis of Small Molecules and Peptides
State-of-the-art chemistry facilities (brand new fumehoods, Buchi rotavapors, vacuum ovens, Biotage Initiator microwave synthesizer, Microsaic MS, HPLC with UV detector (Thermo), etc.) and a last-generation LC-MS (Dionex RSLCnano UPLC) are integrated into a world-class cancer research centre to facilitate the rapid preparation, screening and optimization of novel chemical entities.
The lab specializes on the optimization of kinase inhibitors with suboptimal properties (low solubility, low selectivity, etc.) into drug candidates. By an iterative process that combines ligand-based drug design and highly-focused library synthesis with phenotypic screening, we optimize compounds’ druglikeness at the same time that improve activity and search for novel pharmacological features. This key capability integrates the three themes across the Edinburgh Drug Discovery.
Design and Development of Prodrugs Activated by Metal Implants
The Innovative Therapeutics Lab is pioneering the use of metal catalysts to convert inactive precursors of chemotherapeutics into its active form in a locally-controlled manner. This is based on the capacity of some metal catalysts to be entrapped into biocompatible polymeric devices and remain catalytically active to perform bioorthogonal reactions. The lab provides unique expertise in this emerging field of drug discovery, from the development and screening of novel prodrug strategies for specific applications to the functionalization of different devices with metal catalysts (e.g. palladium).
Target ID and Imaging Tools
The lab designs and develops tailored projects to provide tools for target identification and intracellular imaging by: (i) using bioorthogonal and click chemistry approaches for the functionalization of cell-active small molecules into probes; (ii) functionalizing polymer beads with small molecules to facilitate the capture of target proteins.