Targeting Histone Readers: Non-bromodomain Readers

Le résumé fourni par la source

Histone mark readers have diverse biological functions and dysregulation of these proteins is associated with various diseases. Targeting these readers through therapeutic interventions has become an exciting area of focus in drug discovery. Several modalities have been employed to develop inhibitors against these reader domains, including small molecules and peptides. The optimization of these inhibitors has greatly benefited from the use of structure-based design techniques. In this chapter, we will examine the discovery and development of therapeutics targeting histone non-bromodomain readers, including chromodomains, Tudor domains, PWWP domains, MBT domains, WD40 repeat domains, PHD fingers, and YEATS domains. For each target, we will briefly discuss its identification and biological/biochemical functions before delving into the discovery of inhibitors designed to target these domains. By modulating chromatin dynamics, such inhibitors have the potential to be used as therapeutics for a range of diseases, including cancer and neurological disorders. The search for inhibitors targeting each of these reader domains continues to be an active area of research.

Ce résumé expose les affirmations des auteurs. BNTIC ne l’interprète pas comme une validation indépendante des résultats.