Pushing the boundaries of medicinal chemistry
New drug modalities
Over the past decade, we have observed a shift from traditional small molecule drugs, which activate or repress protein function, to new chemical modalities. Our group believes that some of these modalities could overcome the limitations of conventional drugs against CSCs.
We are pioneering drug strategies that are effective against CSCs only when exposed to light, but remain inactive in the dark. Our vision for the future involves illuminating the tumour to achieve a localised effect, thereby avoiding unwanted effects on stem cells in other tissues and minimising toxic effects in patients.
Ongoing projects
- Development of light-responsive autophagy inhibitors, funded by AECC Ideas Semilla 2024.
Development of photoswitchable FGFR3 inhibitors, funded by Agencia Estatal de Investigación under Proyectos de Generación de Conocimiento 2023.
Publications
- Josa-Culleré, L.; Aira Rodríguez, C.; Llebaria, A. Hemithioindigo-based histone deacetylase inhibitors induce a light-dependent anticancer effect. Eur J Med Chem 2024, 279, 116846. https://doi.org/10.1016/j.ejmech.2024.116846.
- Josa-Culleré, L.; Llebaria, A. Visible-Light-Controlled Histone Deacetylase Inhibitors for Targeted Cancer Therapy. J Med Chem 2023, 66 (3), 1909–1927. https://doi.org/10.1021/acs.jmedchem.2c01713.
Drug delivery strategies based on small molecules
To enhance the selectivity and localisation of drugs against CSCs, we are developing various strategies to guide, accumulate, or release molecules inside these cells through small molecule-based approaches.
Ongoing projects
- Exploiting the activity of the ALDH enzyme to develop highly selective drugs for cancer stem cells, funded by the European Research Council under a Starting Grant 2024.
Medicinal chemistry support
In addition to our primary research lines, we also offer medicinal chemistry support to other research groups. This includes enhancing the activity and properties of hit molecules, identifying bioactive molecules for new targets, or preparing probes for mechanistic studies. We are always open to collaboration, so if you need medicinal chemistry expertise for your projects, do not hesitate to get in touch!
Ongoing projects
- Medicinal chemistry for new inhibitors of TSPAN1 targeting chemoresistant cells in head and neck cancers, in collaboration with Dr Matilde LLeonart (VHIR, Barcelona).
