Dysregulation of the basal RNA polymerase transcription apparatus in cancer
Cet article passe en revue les perspectives offertes par les connaissances récentes sur la structure et la fonction des composants principaux de l'ARN polymérase pour le développement de thérapies ciblées dans divers types de cancers
Mutations that directly affect transcription by RNA polymerases rank among the most central mediators of malignant transformation, but the frequency of new anticancer drugs that selectively target defective transcription apparatus entering the clinic has been limited. This is because targeting the large protein–protein and protein–DNA interfaces that control both generic and selective aspects of RNA polymerase transcription has proved extremely difficult. However, recent technological advances have led to a 'quantum leap' in our comprehension of the structure and function of the core RNA polymerase components, how they are dysregulated in a broad range of cancers and how they may be targeted for 'transcription therapy'.