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Epigenetics-targeted drugs: Current paradigms and future challenges
W Dai, X Qiao, Y Fang, R Guo, P Bai, S Liu… - … and Targeted Therapy, 2024 - nature.com
Epigenetics governs a chromatin state regulatory system through five key mechanisms: DNA
modification, histone modification, RNA modification, chromatin remodeling, and non-coding …
modification, histone modification, RNA modification, chromatin remodeling, and non-coding …
[HTML][HTML] Emerging Targets in Non-Small Cell Lung Cancer
L Liu, J Soler, KL Reckamp, K Sankar - International Journal of Molecular …, 2024 - mdpi.com
Lung cancer is responsible for a high burden of disease globally. Over the last two decades,
the discovery of targetable oncogenic genomic alterations has revolutionized the treatment …
the discovery of targetable oncogenic genomic alterations has revolutionized the treatment …
AMG 193, a clinical stage MTA-cooperative PRMT5 inhibitor, drives antitumor activity preclinically and in patients with MTAP-deleted cancers
B Belmontes, KK Slemmons, C Su, S Liu… - Cancer …, 2025 - aacrjournals.org
One of the most robust synthetic lethal interactions observed in multiple functional genomic
screens has been the dependency on protein arginine methyltransferase 5 (PRMT5) in …
screens has been the dependency on protein arginine methyltransferase 5 (PRMT5) in …
A phase I study to evaluate the safety, pharmacokinetics, and pharmacodynamics of PF-06939999 (PRMT5 inhibitor) in patients with selected advanced or metastatic …
J Rodon, E Rodriguez, ML Maitland, FYC Tsai… - ESMO open, 2024 - Elsevier
Background Protein arginine methyltransferase 5 (PRMT5) methylates multiple substrates
dysregulated in cancer, including spliceosome machinery components. PF-06939999 is a …
dysregulated in cancer, including spliceosome machinery components. PF-06939999 is a …
Transcriptome‐wide gene expression outlier analysis pinpoints therapeutic vulnerabilities in colorectal cancer
E Mariella, G Grasso, M Miotto, K Buzo… - Molecular …, 2024 - Wiley Online Library
Multiple strategies are continuously being explored to expand the drug target repertoire in
solid tumors. We devised a novel computational workflow for transcriptome‐wide gene …
solid tumors. We devised a novel computational workflow for transcriptome‐wide gene …
PRMT5 as a potential therapeutic target in MYC-amplified medulloblastoma
D Kumar, S Jain, DW Coulter, SS Joshi, NK Chaturvedi - Cancers, 2023 - mdpi.com
Simple Summary Medulloblastoma is the most prevalent intracerebellar pediatric brain
tumor, accounting for approximately 20% of all childhood brain tumors and over 60% of …
tumor, accounting for approximately 20% of all childhood brain tumors and over 60% of …
Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity
JM Smith, B Barlaam, D Beattie… - Journal of Medicinal …, 2024 - ACS Publications
PRMT5, a type 2 arginine methyltransferase, has a critical role in regulating cell growth and
survival in cancer. With the aim of develo** MTA-cooperative PRMT5 inhibitors suitable …
survival in cancer. With the aim of develo** MTA-cooperative PRMT5 inhibitors suitable …
Loss of MTAP expression by immunohistochemistry is a surrogate marker for homozygous 9p21. 3 deletion in urothelial carcinoma
T Vlajnic, O Chijioke, L Roma, SS Prince, T Zellweger… - Modern Pathology, 2024 - Elsevier
Homozygous deletion of the chromosomal region 9p21. 3 is common in urothelial carcinoma
(UC) and leads to loss of several genes, including CDKN2A and MTAP, resulting in loss of …
(UC) and leads to loss of several genes, including CDKN2A and MTAP, resulting in loss of …
Type‐I protein arginine methyltransferase inhibition primes anti‐programmed cell death protein 1 immunotherapy in triple‐negative breast cancer
S Zhang, L Guo, Z Zhang, X Liu, W Chen, Y Wei… - Cancer, 2024 - Wiley Online Library
Background Immune‐checkpoint blockade (ICB) therapy shows promise for treating
aggressive triple‐negative breast cancer (TNBC). However, only some patients benefit from …
aggressive triple‐negative breast cancer (TNBC). However, only some patients benefit from …
Synthetic lethal strategies for the development of cancer therapeutics
Synthetic lethality is a genetic phenomenon whereby the simultaneous presence of two
different genetic alterations impairs cellular viability. Importantly, targeting synthetic lethal …
different genetic alterations impairs cellular viability. Importantly, targeting synthetic lethal …