A5100448509- Protein Degradation and Inhibitors
- Histone Deacetylase Inhibitors Research
- Epigenetics and DNA Methylation
- Click Chemistry and Applications
- Multiple Myeloma Research and Treatments
- Ubiquitin and proteasome pathways
- Peptidase Inhibition and Analysis
- Synthesis and biological activity
- Microtubule and mitosis dynamics
- HIV Research and Treatment
- Cancer Genomics and Diagnostics
- HIV/AIDS drug development and treatment
- Computational Drug Discovery Methods
- Cancer-related Molecular Pathways
- Autophagy in Disease and Therapy
- Cancer therapeutics and mechanisms
- RNA Interference and Gene Delivery
- Advanced Breast Cancer Therapies
- Hepatitis C virus research
- Advanced biosensing and bioanalysis techniques
- Chromatin Remodeling and Cancer
- Chemical Synthesis and Analysis
- Bioactive Compounds and Antitumor Agents
- Advancements in Semiconductor Devices and Circuit Design
- Nanoparticle-Based Drug Delivery
Stanford University
2021-2024
Sichuan University
2012-2023
State Key Laboratory of Biotherapy
2012-2023
West China Hospital of Sichuan University
2021-2023
Qilu Hospital of Shandong University
2022
The University of Texas Southwestern Medical Center
2019
Chengdu University
2018
Sichuan Academy of Medical Sciences & Sichuan Provincial People's Hospital
2013
Shanghai Institute of Materia Medica
2010
Chinese Academy of Sciences
2010
The chromosomal theory of inheritance dictates that genes on the same chromosome segregate together while different chromosomes assort independently
Abstract Background Endometrial cancer (EC) is the most common gynecological malignancy in developed countries. Efficacy of bromodomain 4 (BRD4) inhibitor JQ1 has been reported for treatment various human cancers, but its potential impact on EC remains unclear. We therefore aimed to elucidate function BRD4 and effects vivo vitro. Methods The mRNA expression was evaluated using datasets from Cancer Genome Atlas (TCGA) Gene Expression Omnibus (GEO). protein tissues measured...
Abstract Extrachromosomal DNA (ecDNA) presents a major challenge for cancer patients. ecDNA renders tumours treatment resistant by facilitating massive oncogene transcription and rapid genome evolution, contributing to poor patient survival 1–7 . At present, there are no ecDNA-specific treatments. Here we show that enhancing transcription–replication conflict enables targeted elimination of ecDNA-containing cancers. Stepwise analyses reveal pervasive RNA associated single-stranded DNA,...
Over-expressed polo-like kinases 1, a key regulator of cell mitosis, is associated with carcinogenesis and poor prognosis. It very necessary to develop reliable computational affinity prediction protocol targeting PLK1. In this study, the performance different docking scoring function, free energy perturbation, MM-GBSA QM/MM-GBSA were evaluated. The ranking capability FEP best rs = 0.854. However, obtained from can reach 0.767, which requires only about one-eighth simulation time FEP. As for...
Lysine-specific histone demethylase 1 (LSD1) is an attractive target for malignancies therapy. Nevertheless, its role in hepatocellular carcinoma (HCC) progression and the potential of inhibitor HCC therapy remains unclear. Here, we show that LSD1 overexpression human tissues associated with poor patient survival. ZY0511, a highly selective potent LSD1, suppressed cell proliferation vitro tumor growth cell-derived patient-derived xenograft models vivo. Mechanistically, ZY0511 induced mRNA...
Abstract Inflammation is a prevalent pathological process that accompanies the onset and progression of numerous acute chronic diseases including rheumatoid arthritis, sepsis, pancreatitis, atherosclerosis, ischaemic brain/heart disease so forth. However, conventional anti‐inflammatory drugs have certain disadvantages such as nonspecific tissue distribution, low bioavailability, short half‐life, resulting in off‐target side effects limited efficacy control. To address these issues,...
Abstract The bromodomain family member proteins (BRD; BET proteins) are key coregulators for estrogen receptor alpha (ERα)-mediated transcriptional enhancers. use of BRD-selective inhibitors has gained much attention as a potential treatment various solid tumors, including ER-positive breast cancers. However, the roles individual members have largely remained unexplored. Here, we describe role BRDs in (E2)-dependent gene expression ERα-positive cancer cells. We observed that chemical...
Aurora‐A has been known as one of the most important targets for cancer therapy, and some inhibitors have entered clinical trails. In this study, combination ligand‐based structure‐based methods is used to clarify essential quantitative structure–activity relationship inhibitors, multicomplex‐based pharmacophore‐guided method suggested generate a comprehensive pharmacophore kinase based on collection crystal structures Aurora‐A–inhibitor complex. This model successfully identify bioactive...
Aurora and polo-like kinases control the G2/M phase in cell mitosis, which are both considered as crucial targets for cancer proliferations. Here, naphthalene-based Aurora/PLK coinhibitors leading compounds were designed through silico approach, a total of 36 derivatives synthesized. One candidate (AAPK-25) was selected under vitro based high throughput screening with an IC50 value = 0.4 μM to human colon HCT-116. A kinome scan assay showed that AAPK-25 remarkably selective PLK families. The...
PI3Kα (phosphatidylinositol-3-kinase α) and mTOR (the mammalian target of rapamycin) have been treated as anticancer targets in recent years. Since isoform-specific inhibitors may be tolerated at doses that result complete inhibition without generating side effects, a selectivity study is valuable. In this paper, 3D-QSAR CoMFA models on 72 selective were established using the conformations docked to homology models, which show satisfactory linear correlations (PI3Kα: r2 = 0.839, rpred2...
Potent inhibitors of ALK are highly desired because the occurrence drug resistance. We herein firstly report development a rationally designed inhibitor, Con B-1, which can covalently bind to Cys1259, cysteine located outside active site by linking warhead with Ceritinib through 2,2′-Oxybis(ethylamine) linker. The in vitro and vivo assays showed ConB-1 is potent selective ALKi low toxicity normal cells. In addition, molecule significant improvement anticancer activities potential antidrug...
Bromodomain is a recognition module in the signal transduction of acetylated histone. BRD 4, one bromodomain members, emerging as an attractive therapeutic target for several types cancer. Therefore, this study, attempt has been made to screen compounds from integrated database containing 5.5 million 4 inhibitors using pharmacophore‐based virtual screening, molecular docking, and dynamics simulations. As result, two molecules twelve hits were found be active bioactivity tests. Among...