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The interplay between DNA and histone methylation: molecular mechanisms and disease implications
Methylation of cytosine in CpG dinucleotides and histone lysine and arginine residues is a
chromatin modification that critically contributes to the regulation of genome integrity …
chromatin modification that critically contributes to the regulation of genome integrity …
Merging ligand-based and structure-based methods in drug discovery: an overview of combined virtual screening approaches
Virtual screening (VS) is an outstanding cornerstone in the drug discovery pipeline. A variety
of computational approaches, which are generally classified as ligand-based (LB) and …
of computational approaches, which are generally classified as ligand-based (LB) and …
Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease
Protein lysine methylation is a crucial post-translational modification that regulates the
functions of both histone and non-histone proteins. Deregulation of the enzymes or 'writers' …
functions of both histone and non-histone proteins. Deregulation of the enzymes or 'writers' …
A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization
Nuclear receptor-binding SET domain-containing 2 (NSD2) is the primary enzyme
responsible for the dimethylation of lysine 36 of histone 3 (H3K36), a mark associated with …
responsible for the dimethylation of lysine 36 of histone 3 (H3K36), a mark associated with …
Drug discovery targeting nuclear receptor binding SET domain protein 2 (NSD2)
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) …
of histone 3 lysine 36 (H3K36me1 and H3K36me2), using S-adenosyl-l-methionine (SAM) …
The role of NSD1, NSD2, and NSD3 histone methyltransferases in solid tumors
Abstract NSD1, NSD2, and NSD3 constitute the nuclear receptor-binding SET Domain
(NSD) family of histone 3 lysine 36 (H3K36) methyltransferases. These structurally similar …
(NSD) family of histone 3 lysine 36 (H3K36) methyltransferases. These structurally similar …
Discovery of a first-in-class degrader for nuclear receptor binding SET domain protein 2 (NSD2) and Ikaros/Aiolos
Overexpression of nuclear receptor binding SET domain protein 2 (NSD2) is frequent in
multiple myeloma (MM). However, existing NSD2 inhibitors are largely ineffective in …
multiple myeloma (MM). However, existing NSD2 inhibitors are largely ineffective in …
Identification of novel potent NSD2-PWWP1 ligands using structure-based design and computational approaches
L Carlino, PC Astles, B Ackroyd, A Ahmed… - Journal of Medicinal …, 2024 - ACS Publications
Dysregulation of histone methyl transferase nuclear receptor-binding SET domain 2 (NSD2)
has been implicated in several hematological and solid malignancies. NSD2 is a large …
has been implicated in several hematological and solid malignancies. NSD2 is a large …
Evaluating the use of absolute binding free energy in the fragment optimisation process
Key to the fragment optimisation process within drug design is the need to accurately
capture the changes in affinity that are associated with a given set of chemical modifications …
capture the changes in affinity that are associated with a given set of chemical modifications …
Recent advances in nuclear receptor-binding SET domain 2 (NSD2) inhibitors: An update and perspectives
L Zhang, X Zha - European Journal of Medicinal Chemistry, 2023 - Elsevier
Nuclear receptor-binding SET domain 2 (NSD2) is a histone lysine methyltransferase
(HKMTase), which is mainly responsible for the di-methylation of lysine residues on …
(HKMTase), which is mainly responsible for the di-methylation of lysine residues on …