Epigenetic modulations provide multiple levels of regulation mechanisms to fine-tune gene expression and developmental progress without changing the DNA sequence, dysregulation of which lead to various developmental deficiency and diseases. In this thesis, I present the discovery of small molecule inhibitors targeting epigenetic readers: chromodomain (ChD) of chromobox homolog 7 (CBX7) as a histone methylated lysine reader in Chapter II, and bromodomain (BrD) of bromodomain containing 4 (BRD4) as a histone acetylated lysine reader in chapter III respectively. These small molecules may have the potential to be developed into therapeutic compounds to regulate stem cell self-renewal or developmental process, and to treat cancers such as prostate cancer and triple negative breast cancer (TNBC). |