34th Lorne Cancer Conference 2022

Exploiting transcriptional addiction to enhance cancer therapies (#42)

Ricky Johnstone 1 2
  1. The Sir Peter MacCallum Department of Oncology, The University of Melbourne, Melbourne, VIC, Australia
  2. Peter MacCallum Cancer Centre, Melbourne, VIC, Australia

Acurate control of gene-expression is essential for normal development and deregulation of transcription invariably results in human pathologies, including cancer. The dependency of tumour cells on aberrant gene-expression programs and the reliance on core-transcriptional machinery in these cells has been coined “transcriptional addiction”.  Similar to cell cycle regulation, RNA Polymerase II (POLII)-driven transcription should be considered as a unidirectional multistep cycle, consisting of initiation, pausing, elongation, termination and recycling steps, which are tightly controlled by the concerted action of cyclin-dependent kinases (CDKs) and their cognate cyclins, analogous to the cyclin/CDK control of the cell cycle. I will focus on transcriptional CDKs (eg CDK7,8,9,11,12,13) and discuss how dysregulation of the transcription cycle plays an important role in cancer.  I will discuss the development of small molecules targeting transcriptional CDKs as anti-cancer agents and provide a framework for the rational therapeutic application of these agents in oncology.