Category Archives: Thyrotropin-Releasing Hormone Receptors

The Tip60 PDB file was modified in Maestro 9.0.211 to add hydrogen atoms and remove water molecules and the acetyl-CoA from tip60. pathways, including induction of expression of proapoptotic proteins Bax, Bak, PUMA, Noxa, and Bim, and inhibition of expression of antiapoptotic proteins Bcl-2 and Bcl-XL. Anacardic acid was previously exhibited as an inhibitor of DNA polymerase [28]. To develop inhibitors more specifically targeting the MYST family of HATs, our group recently 2′-Deoxyguanosine reported substrate-based analog compounds for Tip60 inhibition [29]. Although they present good inhibition activities, the negative charges due to the presence of CoA motif imply that this type of inhibitors may have low pharmacokinetic performance [30]. To further develop potent inhibitors of MYST HATs with enhanced pharmacological properties, 2′-Deoxyguanosine in this work, we have conducted a virtual screening based on the crystal structure of Esa1 (the yeast homolog of Tip60) to search for small molecule inhibitors. In…

Read more