BRAF inhibitors: from the laboratory to clinical trials

Cet article passe en revue les travaux récents sur le développement d'inhibiteurs de BRAF

Critical Reviews in Oncology/Hematology, sous presse, 2013, résumé

Résumé en anglais

BRAF is one of the most commonly mutated proto-oncogenes and plays a significant role in the development of numerous cancers of high clinical impact. Due to the commonality of BRAF mutations, a number of BRAF inhibitors have been developed as tools in the management of patients with cancers dependent on the action of mutant BRAF to drive cellular proliferation. In this review, we examine the current state of clinical trials and laboratory research concerning BRAF inhibitors in development and available for clinical use. We contrast the effectiveness of type-I and type-II BRAF inhibitors, the former typically showing much more restricted inhibitory selectivity and greater patient response rates.