Protein arginine methylation: from enigmatic functions to therapeutic targeting
Protein arginine methyltransferases (PRMTs) are emerging as attractive therapeutic targets.
PRMTs regulate transcription, splicing, RNA biology, the DNA damage response and cell …
PRMTs regulate transcription, splicing, RNA biology, the DNA damage response and cell …
CARM1 arginine methyltransferase as a therapeutic target for cancer
M Santos, JW Hwang, MT Bedford - Journal of Biological Chemistry, 2023 - ASBMB
Coactivator-associated arginine methyltransferase 1 (CARM1) is an arginine
methyltransferase that posttranslationally modifies proteins that regulate multiple levels of …
methyltransferase that posttranslationally modifies proteins that regulate multiple levels of …
Development of potent and selective coactivator-associated arginine methyltransferase 1 (CARM1) degraders
CARM1 is amplified or overexpressed in many cancer types, and its overexpression
correlates with poor prognosis. Potent small-molecule inhibitors for CARM1 have been …
correlates with poor prognosis. Potent small-molecule inhibitors for CARM1 have been …
The NFIB/CARM1 partnership is a driver in preclinical models of small cell lung cancer
The coactivator associated arginine methyltransferase (CARM1) promotes transcription, as
its name implies. It does so by modifying histones and chromatin bound proteins. We …
its name implies. It does so by modifying histones and chromatin bound proteins. We …
Probing the SAM binding site of SARS-CoV-2 Nsp14 in vitro using SAM competitive inhibitors guides developing selective bisubstrate inhibitors
The COVID-19 pandemic has clearly brought the healthcare systems worldwide to a
breaking point, along with devastating socioeconomic consequences. The SARS-CoV-2 …
breaking point, along with devastating socioeconomic consequences. The SARS-CoV-2 …
BAF155 methylation drives metastasis by hijacking super-enhancers and subverting anti-tumor immunity
Subunits of the chromatin remodeler SWI/SNF are the most frequently disrupted genes in
cancer. However, how post-translational modifications (PTM) of SWI/SNF subunits elicit …
cancer. However, how post-translational modifications (PTM) of SWI/SNF subunits elicit …
Structure-guided design of a selective inhibitor of the methyltransferase KMT9 with cellular activity
S Wang, SO Klein, S Urban, M Staudt… - Nature …, 2024 - nature.com
Inhibition of epigenetic regulators by small molecules is an attractive strategy for cancer
treatment. Recently, we characterised the role of lysine methyltransferase 9 (KMT9) in …
treatment. Recently, we characterised the role of lysine methyltransferase 9 (KMT9) in …
Validating small molecule chemical probes for biological discovery
V Vu, MM Szewczyk, DY Nie… - Annual review of …, 2022 - annualreviews.org
Small molecule chemical probes are valuable tools for interrogating protein biological
functions and relevance as a therapeutic target. Rigorous validation of chemical probe …
functions and relevance as a therapeutic target. Rigorous validation of chemical probe …
Single cell RNA sequencing for breast cancer: present and future
L Ren, J Li, C Wang, Z Lou, S Gao, L Zhao… - Cell Death …, 2021 - nature.com
Breast cancer is one of the most common malignant tumors in women. It is a heterogeneous
disease related to genetic and environmental factors. Presently, the treatment of breast …
disease related to genetic and environmental factors. Presently, the treatment of breast …
Targeting histone modifications in breast cancer: a precise weapon on the way
W Li, H Wu, S Sui, Q Wang, S Xu… - Frontiers in cell and …, 2021 - frontiersin.org
Histone modifications (HMs) contribute to maintaining genomic stability, transcription, DNA
repair, and modulating chromatin in cancer cells. Furthermore, HMs are dynamic and …
repair, and modulating chromatin in cancer cells. Furthermore, HMs are dynamic and …