Discovery of a First-in-Class Degrader for Nuclear Receptor Binding SET Domain Protein 2 (NSD2) and Ikaros/Aiolos

Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease

(2021) Kamakoti P. Bhat et al.   NATURE REVIEWS DRUG DISCOVERY

Discovery of Small-Molecule Antagonists of the PWWP Domain of NSD2

(2021) Renato Ferreira de Freitas et al.   JOURNAL OF MEDICINAL CHEMISTRY

A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization

(2021) David Dilworth et al.   Nature Chemical Biology

Development of a Brigatinib degrader (SIAIS117) as a potential treatment for ALK positive cancer resistance

(2020) Ning Sun et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders

(2020) Meng Cheng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity

(2020) Xuan Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Selective Small Molecule Degraders of BRAF-V600E

(2020) Xiao-Ran Han et al.   JOURNAL OF MEDICINAL CHEMISTRY

Covalent inhibition of NSD1 histone methyltransferase

(2020) Huang Huang et al.   Nature Chemical Biology

Potent and Selective Mitogen-Activated Protein Kinase Kinase 1/2 (MEK1/2) Heterobifunctional Small-molecule Degraders

(2020) Jianping Hu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6

(2019) Baishan Jiang et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Chemoselective Synthesis of Lenalidomide-Based PROTAC Library Using Alkylation Reaction

(2019) Xing Qiu et al.   ORGANIC LETTERS

Understanding histone H3 lysine 36 methylation and its deregulation in disease

(2019) Jie Li et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3

(2019) Jark Böttcher et al.   Nature Chemical Biology

Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader

(2019) Jieli Wei et al.   JOURNAL OF MEDICINAL CHEMISTRY

Histone lysine methyltransferases in biology and disease

(2019) Dylan Husmann et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders

(2018) Mette Ishoey et al.   ACS Chemical Biology

High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2

(2018) Nathan P Coussens et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

BIX-01294 inhibits oncoproteins NSD1, NSD2 and NSD3

(2017) Masayo Morishita et al.   MEDICINAL CHEMISTRY RESEARCH

The Role of Nuclear Receptor–Binding SET Domain Family Histone Lysine Methyltransferases in Cancer

(2017) Richard L. Bennett et al.   Cold Spring Harbor Perspectives in Medicine

Induced protein degradation: an emerging drug discovery paradigm

(2016) Ashton C. Lai et al.   NATURE REVIEWS DRUG DISCOVERY

Catalytic in vivo protein knockdown by small-molecule PROTACs

(2015) Daniel P Bondeson et al.   Nature Chemical Biology

Phthalimide conjugation as a strategy for in vivo target protein degradation

(2015) G. E. Winter et al.   SCIENCE

The NSD family of protein methyltransferases in human cancer

(2015) Theodore Vougiouklakis et al.   Epigenomics

Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia

(2014) B. Xu et al.   BLOOD

Structure-Guided Design and Optimization of Small Molecules Targeting the Protein–Protein Interaction between the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase and the Hypoxia Inducible Factor (HIF) Alpha Subunit with in Vitro Nanomolar Affinities

(2014) Carles Galdeano et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide

(2014) Eric S. Fischer et al.   NATURE

Global chromatin profiling reveals NSD2 mutations in pediatric acute lymphoblastic leukemia

(2013) Jacob D Jaffe et al.   NATURE GENETICS

NSD2 Links Dimethylation of Histone H3 at Lysine 36 to Oncogenic Programming

(2011) Alex J. Kuo et al.   MOLECULAR CELL