Medicinal chemistry strategies targeting PRMT5 for cancer therapy

S Fu, Q Zheng, D Zhang, C Lin, L Ouyang… - European Journal of …, 2022 - Elsevier
Abstract Protein arginine methyltransferases 5 (PRMT5), a therapeutic target whose main
physiological function is mono-and symmetric dimethylation of arginine, has drawn …

[HTML][HTML] Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms

Y Chen, X Shao, X Zhao, Y Ji, X Liu, P Li… - Biomedicine & …, 2021 - Elsevier
The protein arginine methyltransferase 5 (PRMT5) as the major type II arginine
methyltransferase catalyzes the mono-and symmetric dimethylation of arginine residues in …

PRMT5 activates AKT via methylation to promote tumor metastasis

L Huang, XO Zhang, EJ Rozen, X Sun, B Sallis… - Nature …, 2022 - nature.com
Abstract Protein arginine methyltransferase 5 (PRMT5) is the primary methyltransferase
generating symmetric-dimethyl-arginine marks on histone and non-histone proteins. PRMT5 …

CDK5-PRMT1-WDR24 signaling cascade promotes mTORC1 signaling and tumor growth

S Yin, L Liu, LE Ball, Y Wang, MT Bedford, SA Duncan… - Cell reports, 2023 - cell.com
The mammalian target of rapamycin complex1 (mTORC1) is a central regulator of
metabolism and cell growth by sensing diverse environmental signals, including amino …

Autophagy dictates sensitivity to PRMT5 inhibitor in breast cancer

C Brobbey, S Yin, L Liu, LE Ball, PH Howe… - Scientific reports, 2023 - nature.com
Abstract Protein arginine methyltransferase 5 (PRMT5) catalyzes mono-methylation and
symmetric di-methylation on arginine residues and has emerged as a potential antitumor …

Master kinase PDK1 in tumorigenesis

N Zheng, J Wei, D Wu, Y Xu, J Guo - … et Biophysica Acta (BBA)-Reviews on …, 2023 - Elsevier
phosphoinositide-dependent protein kinase 1 (PDK1) is considered as master kinase
regulating AGC kinase family members such as AKT, SGK, PLK, S6K and RSK. Although …

MST2 methylation by PRMT5 inhibits Hippo signaling and promotes pancreatic cancer progression

Y Sun, X Jin, J Meng, F Guo, T Chen, X Zhao… - The EMBO …, 2023 - embopress.org
The Hippo signaling axis is a tumor suppressor pathway that is activated by various extra‐
pathway factors to regulate cell differentiation and organ development. Recent studies have …

The circSPON2/miR-331-3p axis regulates PRMT5, an epigenetic regulator of CAMK2N1 transcription and prostate cancer progression

B Yao, S Zhu, X Wei, MK Chen, Y Feng, Z Li, X Xu… - Molecular Cancer, 2022 - Springer
Abstract Background Prostate cancer (PCa) is the most frequently diagnosed malignancy in
men, and its mechanism remains poorly understood. Therefore, it is urgent to discover …

Arginine methylation of BRD4 by PRMT2/4 governs transcription and DNA repair

L Liu, B Lin, S Yin, LE Ball, JR Delaney, DT Long… - Science …, 2022 - science.org
BRD4 functions as an epigenetic reader and plays a crucial role in regulating transcription
and genome stability. Dysregulation of BRD4 is frequently observed in various human …

A hotspot for posttranslational modifications on the androgen receptor dimer interface drives pathology and anti-androgen resistance

A Alegre-Martí, A Jiménez-Panizo… - Science …, 2023 - science.org
Mutations of the androgen receptor (AR) associated with prostate cancer and androgen
insensitivity syndrome may profoundly influence its structure, protein interaction network …