A5101435119- Peptidase Inhibition and Analysis
- Protein Degradation and Inhibitors
- Ubiquitin and proteasome pathways
- Nanoplatforms for cancer theranostics
- Melanoma and MAPK Pathways
- PARP inhibition in cancer therapy
- Nanoparticle-Based Drug Delivery
- Advanced biosensing and bioanalysis techniques
- DNA Repair Mechanisms
- Epigenetics and DNA Methylation
- Multiple Myeloma Research and Treatments
- Cancer-related Molecular Pathways
- Genomics, phytochemicals, and oxidative stress
- PI3K/AKT/mTOR signaling in cancer
- Soybean genetics and cultivation
- Cancer Mechanisms and Therapy
- Peanut Plant Research Studies
- Plant-derived Lignans Synthesis and Bioactivity
- Graphene and Nanomaterials Applications
- Ferroptosis and cancer prognosis
- Phytochemicals and Antioxidant Activities
- Lung Cancer Treatments and Mutations
- Dendrimers and Hyperbranched Polymers
- Thin-Film Transistor Technologies
- Microbial Metabolism and Applications
First Affiliated Hospital of Xi'an Jiaotong University
2022-2024
Northwestern Polytechnical University
2023-2024
Shaanxi Normal University
2021-2024
Ministry of Education of the People's Republic of China
2023-2024
Jilin Agricultural University
2021
Xi'an Jiaotong University
2010-2019
University of Maryland, Baltimore
2019
Shenyang University of Technology
2009
Developing a sophisticated nanomedicine platform to deliver therapeutics effectively and safely into tumor/cancer cells remains challenging in the field of nanomedicine. In particular, reliable peptide drug delivery systems capable overcoming biological barriers are still lacking. Here, we developed simple, rapid, robust strategy manufacture nanoclusters ∼90 nm diameter that self-assembled from lanthanide-doped nanoparticles (5 nm), two anticancer peptides with different targets (BIM PMI),...
Nanocarrier surface chemistry plays a vital role in mediating cell internalization and enhancing delivery efficiency during vivo chemotherapy. Inspired by the ability of proteins to alter their conformation mediate functions, pH‐/thermal‐/glutathione‐responsive polymer zipper consisting cell‐penetrating poly(disulfide)s thermosensitive polymers bearing guanidinium/phosphate (Gu + /pY − ) motifs spatiotemporally tune composition nanocarriers for precise tumor targeting efficient drug is...
Abstract Androgen receptor splice variant‐7 (AR‐V7), one of the major driving factors, is most attractive drug target in castration‐resistant prostate cancer (CRPC). Currently, no available drugs efficiently AR‐V7 clinical practice. The DNA binding domain (DBD) indispensable for transcriptional activity AR full length and variants, including AR‐V7. Based on homodimerization structure DBD, a novel peptide‐based proteolysis‐targeting chimera (PROTAC) designed to induce degradation DBD...
Peptide drugs offer distinct advantages in therapeutics; however, their limited stability and membrane penetration abilities hinder widespread application. One strategy to overcome these challenges is the hydrocarbon peptide stapling technique, which addresses issues such as poor conformational stability, weak proteolytic resistance, permeability. Nonetheless, while has successfully stabilized α-helical peptides, it shown applicability for most β-sheet motifs. In this study, we present...
Abstract CDK4/6 inhibitors (CDK4/6i) show anticancer activity in certain human malignancies, such as breast cancer. However, their application to other tumor types and intrinsic resistance mechanisms are still unclear. Here, we demonstrate that MYC amplification confers CDK4/6i bladder, prostate cancer cells. Mechanistically, binds the promoter of E3 ubiquitin ligase KLHL42 enhances its transcription, leading RB1 deficiency by inducing both phosphorylated total pRB1 ubiquitination...
While large-scale artificial intelligence (AI) models for protein structure prediction and design are advancing rapidly, the translation of deep learning practical macromolecular drug development remains limited. This investigation aims to bridge this gap by combining cutting-edge methodologies create a novel peptide-based PROTAC paradigm. Using ProteinMPNN RFdiffusion, we identified binding peptides androgen receptor (AR) Von Hippel-Lindau (VHL), followed computational modeling with...
In human mutant BRAF melanoma cells, the stemness transcription factor FOXD3 is rapidly induced by inhibition of ERK1/2 signaling and mediates adaptive resistance to RAF inhibitors. However, mechanism underlying ERK control expression remains unknown. Here we show that SOX10 both necessary sufficient for inhibitor-induced in cells. activates binding a regulatory element promoter. Phosphorylation inhibits its activity toward multiple target genes interfering with sumoylation at K55, which...
Rationale: Although stapled peptides offer a powerful solution to overcome the susceptibility of linear proteolytic degradation and improve their ability cross membranes, an efficient durable disease treatment strategy has not yet been developed due inevitable elimination peptide inhibitors rapid accumulation target proteins.Methods: Herein we peptide-based proteolysis-targeting chimeras (SP-PROTACs), that simultaneously exhibited improved cellular uptake stability attributed peptides,...
Finding the oncogene, which was able to inhibit tumor cells intrinsically and improve immune answers, will be future direction for renal cancer combined treatment. Following patient sample analysis signaling pathway examination, we propose p21-activated kinase 4 (PAK4) as a potential target drug kidney cancer. PAK4 exhibits high expression levels in samples plays regulatory role microenvironment.
Abstract The Bcr/Abl plays a central role in Philadelphia chromosome‐positive (Ph+) leukemia because of the constitutively activated Abl tyrosine kinase and its downstream pathways. Currently, clinical treatment imatinib‐resistant patients with inhibitors is severely limited by drug resistance adverse effects. Herein, dual‐targeting proteolysis‐targeting chimera (PROTAC) protein drug, termed PMI Bcr/Abl‐R6, designed engrafting an MDM2/p53 inhibition peptide sequence onto tetramerization...
Peptides are a rapidly growing class of therapeutics with many advantages over conventional small molecule drugs. Dextrorotary (D)-peptides, increased enzymatic stability and prolonged plasma half-life in comparison natural L-peptides, considered to have great potential as recognition molecules therapeutic agents. However, the vivo efficacy current D-peptides is hindered by their inefficient cellular uptake diseased tissues. Methods: To overcome physiological barriers D-peptides, we designed...
Abstract The mechanistic (formally “mammalian”) target of rapamycin (mTOR) pathway serves as a crucial regulator various biological processes such cell growth and cancer progression. In bladder cancer, recent discoveries showing the cancer-promoting role mTOR complex 1 have attracted wide attention. However, regulation signaling in is complicated underlying mechanism remains elusive. Here, we report that deubiquitinating enzyme, ovarian tumor domain-containing protein 5 (OTUD5), can activate...
Abstract 53BP1 promotes nonhomologous end joining (NHEJ) over homologous recombination (HR) repair by mediating inactivation of DNA resection. Ubiquitination plays an important role in regulating dissociation from double-strand breaks (DSBs). However, how this process is regulated remains poorly understood. Here, we demonstrate that TRABID deubiquitinase binds to at endogenous level and regulates retention DSB sites. deubiquitinates K29-linked polyubiquitination mediated E3 ubiquitin ligase...
Abstract As the world's first oral nuclear export inhibitor, selinexor is increasingly being used in clinical applications for malignant tumors. However, there no extensive exploration on selinexor's adverse events (ADEs), necessitating a real-word assessment of its medication safety. FAERS data (July 2019–June 2023) were searched ADE reports across all indications. Use system organ class (SOC) and preferred terms (PT) from medical dictionary regulatory activities (MedDRA) to describe,...
8501 Background: GSK436 is a highly potent, selective ATP-competitive BRAF inhibitor. BRF112680, first in human study, assessed safety, pharmacokinetics, pharmacodynamics, and efficacy. Efficacy of single-agent was demonstrated V600 mutation-positive (mut+) metastatic melanoma patients (pts), with an unconfirmed response rate (RR) 77% V600E mut+ pts 44% V600K (based on October 2010 data cut). This study evaluates the relationship genetic alterations target genes to RR. Methods: To date,...
Abstract Long non-coding RNAs (lncRNAs) are of more than 200 nucleotides. To date, the roles lncRNAs in soybean fatty acid synthesis have not been fully studied. Here, low-linolenic mutant ‘MT72′ and wild-type control ‘JN18′ were used as materials. The young pods at 30 40 days (d) after flowering systematically identified analyzed using transcriptome sequencing technology combined with bioinformatics tools. A total 39,324 561 differentially expressed identified. lncRNAs-miRNAs-protein-coding...
Photodynamic therapy (PDT) is an appealing treatment modality by producing reactive oxygen species (ROS) with photosensitizers (PSs) to induce cell apoptosis, but still suffering poor efficacy in treating hypoxic solid tumor. Herein, we have developed a nanocarrier (naming HAFeR) encapsulating PSs and RSL3 metal organic framework (MOF) for synergistic ferroptosis PDT. HAFeR nanocarriers selectively recognized CD44 overexpressed on tumor surface, were subsequently internalized via receptor...