Molecule to allow future patient-specific treatment of cancer tumours

Scientists at the Technical University of Munich (TUM) have developed a small, highly active molecule that binds to a specific integrin which operates in many types of cancer

Integrins are links between a cell and its outside world. Cancer cells deploy integrins to break loose from tumour tissue, penetrate blood vessels and ultimately lodge themselves into other tissue as metastases.

However the type of integrin at work can vary from patient to patient.

Tobias Kapp, doctoral candidate in Horst Kessler’s workgroup at the TUM Institute for Advanced Study, said: “If we knew which integrin subtypes are active in the specific cancer of a given patient, we could attack these using appropriate active agents. For this we need compounds that attach to a single integrin as specifically as possible.”

Kessler, Kapp and Oleg Maltsev have successfully developed a ring-shaped compound, which attaches to the alphaVbeta6 integrin, that appears in many different kinds of cancer and also plays a large role in fibroses.

The new molecule selectively docks only to the alphaVbeta6 integrin in cancer, even at relatively low concentrations, making it effective even in small doses, according to MUT.

One of the molecule’s amino acids can also be used as a “hitch” for docking other substances to the compound. Kapp said: “This is of great significance if you want to use the ligands as a diagnostic tool. For example, you can then dock substances that can be made visible using medical imaging equipment.”

In this way tumours can be characterised and then fought using very specifically targeted therapies according to MUT.

Kessler said: "We now know the form of the lock and we know how to make the matching key. This opens the door to a personalised medicine with which we can take patient-specific action against tumour cells."

The results were achieved in the context of a research collaboration between the TUM Department of Chemistry and the TUM University Hospital Klinikum Rechts der Isar, the Università di Napoli Federico II and the Secondo Università di Napoli.