Discovery of Highly Potent, Selective, and Orally Efficacious p300/CBP Histone Acetyltransferases Inhibitors
Yaxi Yang, Rukang Zhang, Zhaojun Li, Lianghe Mei, Shili Wan, Hong Ding, Zhifeng Chen, Jing Xing, Huijin Feng, Jie Han, Hualiang Jiang, Mingyue Zheng, Cheng Luo, Bing Zhou
Abstract
is a highly promising p300/CBP HAT inhibitor and warrants extensive preclinical investigation as a potential clinical development candidate.
Topics & Concepts
CREB-binding proteinHistone AcetyltransferasesChemistryAcetyltransferasesP300-CBP Transcription FactorsAcetylationDrug discoveryHistone acetyltransferaseSmall moleculeHistoneBromodomainCancer researchBiochemistryComputational biologyCREBPharmacologyTranscription factorBiologyGeneProtein Degradation and InhibitorsUbiquitin and proteasome pathwaysGenomics and Chromatin Dynamics