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ESKM, a novel therapeutic agent for sensitive and resistant PH+ leukemias

The mechanism of resistance to JAK2 inhibitor in myeloproliferative neoplasms patients

Effects of PARP inhibitors in BRCA gene-mutated ovarian cancer

DASATINIB; An inhibitor of Receptor Tyrosine Kinase

GP130/JAK/STAT3 signaling pathway induces multiple myeloma

E1 Activating

The Ubiquitin-Proteasome System Facilitates Membrane Fusion and Uncoating during Coronavirus Entry

74 views | Dec 19 2023

Inhibiting the ubiquitin-proteasome system (UPS) at the early infection stage severely impairs the infectivity of Infectious Bronchitis Virus (IBV) and Porcine Epidemic Diarrhea Virus (PEDV) by preventing membrane fusion, uncoating, initial translation, and replication events, highlighting the UPS as a potential target for antiviral therapies against coronaviruses. [Read the Full Post]

Nedd8-Activating Enzyme Is a Druggable Host Dependency Factor of Human and Mouse Cytomegalovirus

132 views | Sep 02 2023

The study suggests that the Nedd8-activating enzyme (NAE), the neddylation process, and cullin RING ubiquitin ligases (CRLs) are potential targets for developing drugs against cytomegalovirus infections. [Read the Full Post]

Effects of arsenic on the topology and solubility of promyelocytic leukemia (PML)-nuclear bodies

78 views | Aug 21 2023

Trivalent arsenic (As3+) induces a solubility shift in PML, leading to rapid SUMOylation and late agglomeration of PML nuclear bodies (PML-NBs), which has implications for the regulation of intranuclear dynamics in the context of acute promyelocytic leukemia (APL). [Read the Full Post]

Proteasomal pathway inhibition as a potential therapy for NF2-associated meningioma and schwannoma

82 views | Jul 29 2023

This study highlights the potential of proteasome pathway inhibitors, specifically ixazomib and TAK-243, as novel and promising therapies for NF2-associated tumors, demonstrating efficacy in preclinical models and laying the groundwork for future clinical investigations. [Read the Full Post]

UBA1 inhibition contributes radiosensitization of glioblastoma cells via blocking DNA damage repair

111 views | Jul 29 2023

The study demonstrated that the UBA1 inhibitor TAK-243, in combination with ionizing radiation, effectively inhibited GBM cell proliferation, impaired DNA double-strand break repair, and increased apoptosis, providing a potential therapeutic approach to enhance the radiation sensitivity of GBM. [Read the Full Post]

Early growth response-1 is a new substrate of the GSK3β-FBXW7 axis

56 views | Oct 17 2022

Lu Yin et al. found that EGR1 was a new substrate of the GSK3β-FBXW7 axis, and the FBXW7-EGR1 axis coordinately regulated growth of cancer cells. [Read the Full Post]

Phase 1 study to evaluate the effects of rifampin on pharmacokinetics of pevonedistat, a NEDD8-activating enzyme inhibitor in patients with advanced solid tumors

61 views | Aug 17 2022

Xiaofei Zhou et al, supported the recommendation that no pevonedistat dose adjustment was needed for patients receiving concomitant CYP3A inducers. [Read the Full Post]

Neddylation is essential for β-catenin degradation in Wnt signaling pathway

313 views | Apr 10 2022

Bojun Wang et al. highlighted the importance of reassessing previously identified ubiquitylation substrates. [Read the Full Post]

GRP78 blockade overcomes intrinsic resistance to UBA1 inhibitor TAK-243 in glioblastoma

284 views | Apr 10 2022

Xu Zhang et al. provided a new strategy for improving the sensitivity of GBM to TAK-243 treatment and experimental basis for further clinical trials to evaluate this combination therapy. [Read the Full Post]

Blocking neddylation elicits antiviral effect against hepatitis B virus replication

214 views | Nov 23 2021

Karima Abounouh et al. provided new tools interfering with HBV persistence as well as novel therapeutic strategies against chronic hepatitis B. [Read the Full Post]