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PRMT

Discovery and Pharmacological Characterization of JNJ-64619178, a Novel Small-Molecule Inhibitor of PRMT5 with Potent Antitumor Activity

59 views | Mar 08 2022

Dirk Brehmer et al. supported the continued clinical evaluation of JNJ-64619178 in patients with aberrant PRMT5 activity-driven tumors. [Read the Full Post]

EPZ015666, a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an antitumour effect in retinoblastoma

0 views | Jan 23 2022

Xing Liu et al. found that PRMT5 promoted retinoblastoma growth, the PRMT5 inhibitor EPZ015666 inhibited retinoblastoma in vitro by regulating P53-P21/P27-CDK2 signaling pathways and slowed retinoblastoma growth in a xenograft model. [Read the Full Post]

Protein Arginine Methyltransferase 5 Promotes the Migration of AML Cells by Regulating the Expression of Leukocyte Immunoglobulin-Like Receptor B4

99 views | Jan 22 2022

Lu Zhao found that PRMT5 plays an important role in the invasion of AML, which acts via regulating the expression of LILRB4. PRMT5 could act as a potential therapeutic candidate for AML. Copyright © 2021 Lu Zhao et al. [Read the Full Post]

Myelocytomatosis-Protein Arginine N-Methyltransferase 5 Axis Defines the Tumorigenesis and Immune Response in Hepatocellular Carcinoma

326 views | Aug 24 2021

Yuhong Luo et al. revealed that PRMT5 was an epigenetic executer of MYC, leading to repression of the transcriptional regulation of downstream genes that promoted hepatocellular carcinogenesis. [Read the Full Post]

Rational Design, synthesis and biological evaluation of novel triazole derivatives as potent and selective PRMT5 inhibitors with antitumor activity

294 views | Mar 21 2021

Kongkai Zhu et al. described the design, synthesis and biological evaluation of a series of novel, potent and selective PRMT5 inhibitors with antiproliferative activity against Z-138 mantle cell lymphoma cell line. [Read the Full Post]

Inhibition of PRMT5 Attenuates Oxidative Stress-Induced Pyroptosis via Activation of the Nrf2/HO-1 Signal Pathway in a Mouse Model of Renal Ischemia-Reperfusion Injury

331 views | Jan 29 2021

Changhui Diao et al. thought that PRMT5 might be a promising therapeutic target. [Read the Full Post]

EPZ015666, a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an antitumour effect in retinoblastoma

373 views | Jan 29 2021

Xing Liu et al. found that EPZ015666 inhibited retinoblastoma cell proliferation and led to cell cycle arrest at the G1 phase. [Read the Full Post]

PRMT5 control of cGAS/STING and NLRC5 pathways defines melanoma response to antitumor immunity

429 views | Aug 03 2020

Hyungsoo Kim et al. provided a rationale to test PRMT5 inhibitors in immunotherapy-based clinical trials as a means to enhance an antitumor immune response. [Read the Full Post]

Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma

544 views | Oct 16 2019

AbuHammad S et al. provided a strong rationale for further investigation of novel combinations of CDK4/6 and PRMT5 inhibitors, not only in melanoma but other tumor types, including breast, pancreatic, and esophageal carcinoma. [Read the Full Post]

A patent review of arginine methyltransferase inhibitors (2010-2018)

599 views | Jul 10 2019

Li X et al. summarized the updated patented inhibitors targeting PRMTs from 2010 to 2018. The authors illustrate the chemical structures, molecular mechanism of action, pharmacological activities as well as the potential clinical application including combination therapy and biomarker-guided therapy. PRMT inhibitors in clinical trials are also highlighted. The authors provide a future perspective for further development of potent and selective PRMT inhibitors. [Read the Full Post]