Due to their prevalent role in epigenetic gene regulation, methyllysine and methylarginine domain readers have emerged as potential drug targets for small-molecule intervention. Within this book chapter, the biological role and the associated development of potent small molecules inhibiting the protein-protein interaction of methyllysine readers (Tudor, malignant brain tumor, chromo-, and PHD domain) will be discussed. The druggability of these readers and thus their potential to serve as targets for small-molecule ligands will be evaluated critically. Those domains (PWWP, WD40, ankyrin repeats, and ADD domains) which are not yet targeted will be evaluated for their biological actions and eventual therapeutic implications. To sum up, a comprehensive review of the state of the art for all relevant methyl-readers and their inhibitors if present will be given from a medicinal chemistry standpoint of view.
Methyl-Readers and Inhibitors
Sbardella, Gianluca
2020
Abstract
Due to their prevalent role in epigenetic gene regulation, methyllysine and methylarginine domain readers have emerged as potential drug targets for small-molecule intervention. Within this book chapter, the biological role and the associated development of potent small molecules inhibiting the protein-protein interaction of methyllysine readers (Tudor, malignant brain tumor, chromo-, and PHD domain) will be discussed. The druggability of these readers and thus their potential to serve as targets for small-molecule ligands will be evaluated critically. Those domains (PWWP, WD40, ankyrin repeats, and ADD domains) which are not yet targeted will be evaluated for their biological actions and eventual therapeutic implications. To sum up, a comprehensive review of the state of the art for all relevant methyl-readers and their inhibitors if present will be given from a medicinal chemistry standpoint of view.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
