Glutaminase

Novel Glutamine Antagonist JHU395 Suppresses MYC-Driven Medulloblastoma Growth and Induces Apoptosis

29 views | Nov 03 2023

The preclinical study demonstrated that the brain-targeted prodrug JHU395, derived from the glutamine antagonist 6-diazo-5-oxo-l-norleucine (DON), effectively killed MYC-expressing medulloblastoma cells, increased survival in mice with MYC-amplified medulloblastoma tumors, and showed promise for further development as a potential treatment for medulloblastoma. [Read the Full Post]

H1N1 influenza virus infection through NRF2-KEAP1-GCLC pathway induces ferroptosis in nasal mucosal epithelial cells

111 views | Sep 06 2023

This study reveals that the H1N1 virus induces ferroptosis in human nasal epithelial cells via the NRF2-KEAP1-GCLC signaling pathway and glutaminolysis, contributing to nasal mucosal epithelial inflammation and suggesting a potential therapeutic target for viral-induced nasal inflammation. [Read the Full Post]

Deciphering the mechanism of PSORI-CM02 in suppressing keratinocyte proliferation through the mTOR/HK2/glycolysis axis

109 views | Jun 26 2023

PSORI-CM02 exhibits anti-proliferative effects on psoriatic keratinocytes by inhibiting the mTOR/HK2/glycolysis axis, as demonstrated in both in vitro and in vivo models. [Read the Full Post]

Characterization of cell line with dedifferentiated GIST-like features established from cecal GIST of familial GIST model mice

69 views | Jun 21 2023

The study established a cell line derived from cecal GIST in a familial GIST mouse model, characterized as dedifferentiated GIST-like cells with high expression of HSP90 families and glutaminase 1, and identified the combination of Pimitespib and Telaglenastat as a potential treatment strategy for these cells. [Read the Full Post]

CD133-Functionalized Gold Nanoparticles as a Carrier Platform for Telaglenastat (CB-839) against Tumor Stem Cells

137 views | May 29 2022

Elham Poonaki et al. showed that Au-PEG-CD133-CB-839 significantly decreased the viability of CD133-postive cancer cells in a dose-dependent manner, which was higher as compared to the effects of treatment of the cells with the individual components of the assembled nanodrug. [Read the Full Post]

Biomarker guided treatment in oncogene-driven advanced non-small cell lung cancer in older adults: A Young International Society of Geriatric Oncology Report

130 views | May 11 2022

Konstantinos Christofyllakis et al. thought that molecularly-guided therapy for most alterations was safe and efficacious in older adults with oncogene-driven advanced NSCLC. [Read the Full Post]

Impaired anaplerosis is a major contributor to glycolysis inhibitor toxicity in glioma

381 views | Jul 09 2021

Sunada Khadka et al. suggested that at least for ENO1-deleted gliomas, tumors in vivo-unlike cells in culture-show limited dependence on glutaminolysis and instead primarily depended on glycolysis for anaplerosis. [Read the Full Post]

Pyruvate Anaplerosis Is a Mechanism of Resistance to Pharmacological Glutaminase Inhibition in Triple-Receptor Negative Breast Cancer

422 views | Jun 02 2020

Dean C Singleton et al. highlighted the potential influence that both circulating and tumour-derived pyruvate could have on glutaminase inhibitor efficacy. Furthermore, they highlighted the benefits of 3D spheroid cultures to model the features of the tumour microenvironment and improved the in vitro investigation of cancer metabolism-targeted therapeutics. [Read the Full Post]

Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer

457 views | Jul 29 2019

Gross MI et al. provided a strong rationale for the clinical investigation of CB-839 as a targeted therapeutic in patients with TNBC and other glutamine-dependent tumors. [Read the Full Post]

Glutaminase inhibitor CB-839 synergizes with carfilzomib in resistant multiple myeloma cells

574 views | Feb 03 2019

Thompson RM et al. suggested that the acquisition of PI resistance involves adaptations in cellular bioenergetics, supporting the combination of CB-839 with Crflz for the treatment of refractory MM. [Read the Full Post]