|Awarded On||February 21, 2018|
|Title||Novel Small Molecule Probes Targeting Histone Acetyltransferase p300/CBP|
|Award Mechanism||Individual Investigator|
|Institution/Organization||Baylor College of Medicine|
|Principal Investigator/Program Director||Yongcheng Song|
Human genome is composed of double-stranded DNA wrapped around millions of protein histone cores. Acetylation of histones plays critical roles in gene transcription, DNA replication and repair. In addition, aberrant histone acetylation often occurs in many diseases such as cancer. In this project, we aim to discover and develop novel small molecule inhibitors of histone acetyltransferases (HAT) p300 and CBP, which are proteins that can acetylate histones and are co-activators of gene transcription. Previous studies have shown HAT activity of p300/CBP is essential for many transcription factors mediated gene transcription as well as oncogene driven cancers, including ~15% acute myeloid leukem...