Understanding histone H3 lysine 36 methylation and its deregulation in disease

J Li, JH Ahn, GG Wang - Cellular and Molecular Life Sciences, 2019 - Springer
Methylation of histone H3 lysine 36 (H3K36) plays crucial roles in the partitioning of
chromatin to distinctive domains and the regulation of a wide range of biological processes …

The role of NSD1, NSD2, and NSD3 histone methyltransferases in solid tumors

I Topchu, RP Pangeni, I Bychkov, SA Miller… - Cellular and Molecular …, 2022 - Springer
Abstract NSD1, NSD2, and NSD3 constitute the nuclear receptor-binding SET Domain
(NSD) family of histone 3 lysine 36 (H3K36) methyltransferases. These structurally similar …

Molecular basis of nucleosomal H3K36 methylation by NSD methyltransferases

W Li, W Tian, G Yuan, P Deng, D Sengupta, Z Cheng… - Nature, 2021 - nature.com
Histone methyltransferases of the nuclear receptor-binding SET domain protein (NSD)
family, including NSD1, NSD2 and NSD3, have crucial roles in chromatin regulation and are …

Discovery of a potent and selective targeted NSD2 degrader for the reduction of H3K36me2

RP Hanley, DY Nie, JR Tabor, F Li… - Journal of the …, 2023 - ACS Publications
Nuclear receptor-binding SET domain-containing 2 (NSD2) plays important roles in gene
regulation, largely through its ability to dimethylate lysine 36 of histone 3 (H3K36me2) …

Covalent inhibition of NSD1 histone methyltransferase

H Huang, CA Howard, S Zari, HJ Cho, S Shukla… - Nature chemical …, 2020 - nature.com
The nuclear receptor-binding SET domain (NSD) family of histone methyltransferases is
associated with various malignancies, including aggressive acute leukemia with NUP98 …

[HTML][HTML] An OpenData portal to share COVID-19 drug repurposing data in real time

KR Brimacombe, T Zhao, RT Eastman, X Hu, K Wang… - BioRxiv, 2020 - ncbi.nlm.nih.gov
Abstract The National Center for Advancing Translational Sciences (NCATS) has developed
an online open science data portal for its COVID-19 drug repurposing campaign–named …

Discovery of a first-in-class degrader for nuclear receptor binding SET domain protein 2 (NSD2) and Ikaros/Aiolos

F Meng, C Xu, KS Park, HU Kaniskan… - Journal of medicinal …, 2022 - ACS Publications
Overexpression of nuclear receptor binding SET domain protein 2 (NSD2) is frequent in
multiple myeloma (MM). However, existing NSD2 inhibitors are largely ineffective in …

Hydrophobic tag tethering degrader as a promising paradigm of protein degradation: past, present and future perspectives

S Ha, J Zhu, H Xiang, G Luo - Chinese Chemical Letters, 2024 - Elsevier
Small molecule inhibitors have dominated the pharmaceutical landscape for a long time as
the primary therapeutic paradigm targeting pathogenic proteins. However, their efficacy …

Drug discovery targeting nuclear receptor binding SET domain protein 2 (NSD2)

Z Ma, AA Bolinger, H Chen, J Zhou - Journal of medicinal …, 2023 - ACS Publications
Nuclear receptor binding SET domain proteins (NSDs) catalyze the mono-or dimethylation
of histone 3 lysine 36 (H3K36me1 and H3K36me2), using S-adenosyl-l-methionine (SAM) …

Nuisance compounds in cellular assays

JL Dahlin, DS Auld, I Rothenaigner, S Haney… - Cell chemical …, 2021 - cell.com
Compounds that exhibit assay interference or undesirable mechanisms of bioactivity ("
nuisance compounds") are routinely encountered in cellular assays, including phenotypic …