Concepedia

Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors

Rukang Zhang, Zhaojun Li, Lianghe Mei, Shili Wan, Hong Ding, Zhifeng Chen, Jing Xing, Huijin Feng, Jie Han, Hualiang Jiang,

Journal of Medicinal Chemistry · 2020 · 131 citations · 38 references

DOIFull text

Open access

Concepts

Abstract

is a highly promising p300/CBP HAT inhibitor and warrants extensive preclinical investigation as a potential clinical development candidate.

References

38

Super-Enhancers in the Control of Cell Identity and Disease

Denes Hnisz, Brian J. Abraham, Tong Ihn Lee et al. · Cell · 2013 · 3.9K citations · Full text

, , +9

The Transcriptional Coactivators p300 and CBP Are Histone Acetyltransferases

Vasily Ogryzko, R. Louis Schiltz, Valya Russanova et al. · Cell · 1996 · 3K citations · Full text

, , +13

Activation of p53 Sequence-Specific DNA Binding by Acetylation of the p53 C-Terminal Domain

Wei Gu, R G Roeder · Cell · 1997 · 2.6K citations · Full text

, , +12

Monitoring Drug Target Engagement in Cells and Tissues Using the Cellular Thermal Shift Assay

Daniel Martinez Molina, Rozbeh Jafari, Marina Ignatushchenko et al. · Science · 2013 · 2.2K citations

, , +17

The CBP co-activator is a histone acetyltransferase

Andrew J. Bannister, Tony Kouzarides · Nature · 1996 · 1.8K citations

, , +11