Discovery of linear unnatural peptides as potent mutant isocitrate dehydrogenase 1 inhibitors by Ugi reaction

1 views | Jan 23 2022

Xuechen Zhou et al. found that IDH1could decrease the cellular concentration of 2-HG, and suppress the proliferation of HT1080 and IDH1 mutant-U-87 cells by selectively inhibiting the activity of mutant IDH1. [Read the Full Post]

Dual-Knockout of Mutant Isocitrate Dehydrogenase 1 and 2 Subtypes Towards Glioma Therapy: Structural Mechanistic Insights on the Role of Vorasidenib

3 views | Jan 17 2022

Preantha Poonan et al. provided thorough structural and dynamic insights associated with the dual inhibitory activity of AG-881 towards glioma therapy. [Read the Full Post]

Vorasidenib, a Dual Inhibitor of Mutant IDH1/2, in Recurrent or Progressive Glioma; Results of a First-in-Human Phase I Trial

4 views | Jan 17 2022

Ingo K Mellinghoff et al. found that vorasidenib was well tolerated and showed preliminary antitumor activity in patients with recurrent or progressive nonenhancing mIDH LGG. [Read the Full Post]

ALDH1A1 maintains the cancer stem-like cells properties of esophageal squamous cell carcinoma by activating the AKT signal pathway and interacting with β-catenin

137 views | Mar 18 2021

Wei Wang et al. found that ALDH1A1 expression maintained the CSC properties of ESCC cells. [Read the Full Post]

Population pharmacokinetic and exposure-response analyses of ivosidenib in patients with IDH1-mutant advanced hematologic malignancies

148 views | Jan 30 2021

Xuemin Jiang et al. provided a framework to describe the relationship among ivosidenib dose, exposure, and clinical end points. [Read the Full Post]

MR-detectable metabolic biomarkers of response to mutant IDH inhibition in low-grade glioma

151 views | Jan 25 2021

Abigail R Molloy et al. identified potential 1H- and 13C-MRS-detectable biomarkers of response to IDH1mut inhibition in gliomas. [Read the Full Post]

Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of Glioma

173 views | Jan 25 2021

Zenon Konteatis et al. described the discovery of vorasidenib (AG-881), a potent, oral, brain-penetrant dual inhibitor of both mIDH1 and mIDH2. [Read the Full Post]

Targeting the epigenome: Screening bioactive compounds that regulate histone deacetylase activity

0 views | Jan 30 2019

Godoy LD et al. provided the first step in identifying multiple bioactive compound HDAC inhibitors. [Read the Full Post]

Cell-based assay system for high-throughput screening of anti-photo-aging agents in fibroblast transfectants

0 views | Dec 21 2018

Lee S et al. revealed that CCN1-GFs treated with sclareol showed decreased levels of UVB-induced CCN1 expression. [Read the Full Post]

A sensitive virus yield assay for evaluation of Antivirals against Zika Virus

0 views | Nov 26 2018

Goebel S et al. indicated that due to reproducible assay performance, qPCR associated higher sensitivity and short duration of the assay time, this novel cell based assay will be very useful for confirming the activity of antivirals against ZIKV. [Read the Full Post]