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

KP Bhat, H Ümit Kaniskan, J Jin… - Nature Reviews Drug …, 2021 - nature.com
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' …

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) …

A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization

D Dilworth, RP Hanley, R Ferreira de Freitas… - Nature chemical …, 2022 - nature.com
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 …

A specific G9a inhibitor unveils BGLT3 lncRNA as a universal mediator of chemically induced fetal globin gene expression

S Takase, T Hiroyama, F Shirai, Y Maemoto… - Nature …, 2023 - nature.com
Sickle cell disease (SCD) is a heritable disorder caused by β-globin gene mutations.
Induction of fetal γ-globin is an established therapeutic strategy. Recently, epigenetic …

CACHE Challenge# 1: targeting the WDR domain of LRRK2, a Parkinson's Disease associated protein

F Li, S Ackloo, CH Arrowsmith, F Ban… - Journal of Chemical …, 2024 - ACS Publications
The CACHE challenges are a series of prospective benchmarking exercises to evaluate
progress in the field of computational hit-finding. Here we report the results of the inaugural …

Multifaceted role of PRDM proteins in human cancer

A Casamassimi, M Rienzo, E Di Zazzo… - International Journal of …, 2020 - mdpi.com
The PR/SET domain family (PRDM) comprise a family of genes whose protein products
share a conserved N-terminal PR [PRDI-BF1 (positive regulatory domain I-binding factor 1) …

Subpocket similarity-based hit identification for challenging targets: Application to the WDR domain of LRRK2

M Eguida, G Bret, F Sindt, F Li, I Chau… - Journal of Chemical …, 2024 - ACS Publications
We herewith applied a priori a generic hit identification method (POEM) for difficult targets of
known three-dimensional structure, relying on the simple knowledge of physicochemical …

Chemical biology and pharmacology of histone lysine methylation inhibitors

SH Barghout, RAC Machado… - Biochimica et Biophysica …, 2022 - Elsevier
Histone lysine methylation is a post-translational modification that plays a key role in the
epigenetic regulation of a broad spectrum of biological processes. Moreover, the …

Targeting Alpha‐Ketoglutarate Disruption Overcomes Immunoevasion and Improves PD‐1 Blockade Immunotherapy in Renal Cell Carcinoma

L Li, X Zeng, Z Chao, J Luo, W Guan… - Advanced …, 2023 - Wiley Online Library
The Warburg effect‐related metabolic dysfunction of the tricarboxylic acid (TCA) cycle has
emerged as a hallmark of various solid tumors, particularly renal cell carcinoma (RCC). RCC …

Meiotic genes and DNA double strand break repair in cancer

L Lingg, S Rottenberg, P Francica - Frontiers in genetics, 2022 - frontiersin.org
Tumor cells show widespread genetic alterations that change the expression of genes
driving tumor progression, including genes that maintain genomic integrity. In recent years, it …