Receptor tyrosine kinases: Characterisation, mechanism of action and therapeutic interests for bone cancers

J Bone Oncol · 2015 · Classic · cited 159 times

Aude I. Ségaliny, Marta Tellez Gabriel, Marie‐Françoise Heymann, Dominique Heymann

Orthopaedic Oncology

SUMMARY — THE REDUCTIONThis 2015 review examines receptor tyrosine kinases and RTK inhibitors as therapeutic targets in bone sarcomas and bone metastases, building on successes like imatinib in other cancers.
Abstract, as published

Bone cancers are characterised by the development of tumour cells in bone sites, associated with a dysregulation of their environment. In the last two decades, numerous therapeutic strategies have been developed to target the cancer cells or tumour niche. As the crosstalk between these two entities is tightly controlled by the release of polypeptide mediators activating signalling pathways through several receptor tyrosine kinases (RTKs), RTK inhibitors have been designed. These inhibitors have shown exciting clinical impacts, such as imatinib mesylate, which has become a reference treatment for chronic myeloid leukaemia and gastrointestinal tumours. The present review gives an overview of the main molecular and functional characteristics of RTKs, and focuses on the clinical applications that are envisaged and already assessed for the treatment of bone sarcomas and bone metastases.

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