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CD74-ROS1 G2032R mutation transcriptionally up-regulates Twist1 in non-small cell lung cancer cells leading to increased migration, invasion, and resistance to crizotinib.
TLDR
Results suggested that CD74-ROS1 G2032R mutation mediated EMT phenotype by increasing the expression of Twist1, resulting in drug resistance, may provide a potent strategy to treat the ROS1+ NSCLC patients with crizotinib resistance.
Titanium dioxide nanoparticles induce mouse hippocampal neuron apoptosis via oxidative stress- and calcium imbalance-mediated endoplasmic reticulum stress.
TLDR
The study suggests that TiO2-NPs-induced apoptosis in HT22 cells is through oxidative stress- and calcium imbalance-mediated ERS, which is related to endoplasmic reticulum stress.
Design, synthesis and biological evaluation of novel 4-anilinoquinazoline derivatives as hypoxia-selective EGFR and VEGFR-2 dual inhibitors.
TLDR
The results suggest that EGFR/VEGFR-2 dual inhibitors, 10a and 10g, emerged as potential hypoxia-selective anti-tumor drugs with less toxicity for inhibiting in vitro and vivo models of non-small cell lung cancer cells.
Discovery of novel 2,4-diarylaminopyrimidine analogues as ALK and ROS1 dual inhibitors to overcome crizotinib-resistant mutants including G1202R.
TLDR
34c was potent against a variety of frequently observed crizotinib-resistant mutants, particularly the L1196M mutant identified as the "gatekeeper" mutation and the G1202R mutant which conferred resistance to all clinical stage ALK inhibitors.
Decreased expression of BTG3 was linked to carcinogenesis, aggressiveness, and prognosis of ovarian carcinoma
TLDR
B-cell translocation gene 3 (BTG3) is a member of the BTG family which inhibits cell proliferation, metastasis, and angiogenesis, and also regulates cell-cycle progression and differentiation in a variety of cell types and is considered as a good marker to indicate the favorable prognosis of EOCs.
Dual potent ALK and ROS1 inhibitors combating drug-resistant mutants: Synthesis and biological evaluation of aminopyridine-containing diarylaminopyrimidine derivatives.
TLDR
F-1 was capable of suppressing phospho-ALK and its relative downstream signaling pathways, and eventually, inducing cell apoptosis in a dose-dependent manner in Karpas-299 cell, validated as a promising ALK/ROS1 dual inhibitor great potential for G1202R ALK mutation cancers.
Acetaldehyde Induces Neurotoxicity In Vitro via Oxidative Stress- and Ca2+ Imbalance-Mediated Endoplasmic Reticulum Stress
TLDR
It is found that ADE exhibited cytotoxicities against HT22 cells and primary cultured cortical neuronal cells in dose-dependent manners and induced apoptosis of HT 22 cells by upregulating the expression of caspase family proapoptotic proteins.
2-Methoxy-5((3,4,5-trimethosyphenyl)seleninyl) phenol reverses EGF-induced cell migration and invasion through down-regulation of MDM2 in breast cancer cell lines
TLDR
It is found that SQ reversed epidermal growth factor (EGF)-induced motility and invasion in breast cancer cell lines by the in vitro Wound healing and Transwell assay and suggest that the inhibitory effects of SQ on migration and invasion were related to the suppression of MDM2 and Twist1 signal axis.
Ursolic acid derivative UA232 evokes apoptosis of lung cancer cells induced by endoplasmic reticulum stress
TLDR
UA232 induced apoptosis through the ER stress pathway, and showed stronger growth-inhibitory effects in A549 and H460 cells compared to UA, which may be a potential anticancer drug to suppress the proliferation of lung cancer.
Recent progress in small-molecule inhibitors for critical therapeutic targets of necroptosis.
TLDR
A list of the known small-molecule inhibitors of these enzymes and representative structures of compounds co-crystallized with these proteins and put forward some thoughts regarding their future development are compiled.
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