Journal of medicinal chemistryHistone-Lysine N-MethyltransferaseHumansLigandsStructure-Activity RelationshipDNA
Fragment-Based Screening of NSD2-PWWP1 Identifies Novel Covalent Allosteric Ligands That Diminish Methyllysine and DNA Binding Abilities of NSD2.
Yunyuan Huang, Yanxi Li, Xin Chen, Huiling Wang, Qian Wang, Siying Liu, Yigui Li, Zhuo Chen, Jun Ma, Zeyue Huang, Jian Wan, Yanliang Ren, Jinrong Min
Published: 202510.1021/acs.jmedchem.5c01902
Abstract
The PWWP1 domain of NSD2 recognizes both H3K36me2/3 and DNA, a function critical for its subcellular localization and oncogenic activity, making it a promising therapeutic target. In this study, through fragment library screening and structure-activi…
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