Chapter 15: Chromatin Remodeling Complexes: Arising Opportunities and Challenges of Targeting Chromatin Remodelers

Chromatin remodeling complexes are the gatekeepers of chromatin accessibility and subsequent activation or repression of transcriptional programs. They have essential functions and aberrant activity due to mutations or loss of function of key components is often found associated with diseases, notably cancer and immunological disorders. In this chapter we highlight the diverse ways in which chromatin remodeling complexes can be targeted specifically with a focus towards development of therapeutics using multiple drug discovery approaches including inhibition, targeted protein degradation, and protein–protein interaction (PPI) disruption of transcription factor binding to remodeling complexes. With these varied strategies, targeted therapies for numerous diseases which are driven by inappropriate chromatin remodeling activity can be developed impacting the lives of significant numbers of patients.