A5100394873- Metal complexes synthesis and properties
- Drug Transport and Resistance Mechanisms
- Lung Cancer Research Studies
- Synthesis of Tetrazole Derivatives
- Chemokine receptors and signaling
- Cytokine Signaling Pathways and Interactions
- Peptidase Inhibition and Analysis
- Immune Cell Function and Interaction
- DNA and Nucleic Acid Chemistry
- Neuroendocrine Tumor Research Advances
- HER2/EGFR in Cancer Research
- Cancer Mechanisms and Therapy
- Metal-Organic Frameworks: Synthesis and Applications
- Magnetism in coordination complexes
- Lung Cancer Treatments and Mutations
- Diabetes Treatment and Management
- PARP inhibition in cancer therapy
- Colorectal and Anal Carcinomas
- Cutaneous Melanoma Detection and Management
- Synthesis and biological activity
- Rheumatoid Arthritis Research and Therapies
- Nonmelanoma Skin Cancer Studies
- Synthesis and Characterization of Heterocyclic Compounds
- RNA Research and Splicing
- Cancer Immunotherapy and Biomarkers
Beijing Luhe Hospital Affiliated to Capital Medical University
2024
University of Chinese Academy of Sciences
2024
Shanghai Institute of Materia Medica
2013-2024
Chinese Academy of Sciences
2024
Jiangsu T-mab BioPharma (China)
2024
Chinese People's Armed Police General Hospital
2024
Chinese People's Armed Police Force
2024
Sichuan Cancer Hospital
2022-2023
University of Electronic Science and Technology of China
2022-2023
Henan Provincial People's Hospital
2023
Specialized chromatin structures such as nucleosomes with specific histone modifications decorate exons in eukaryotic genomes, suggesting a functional connection between organization and the regulation of pre-mRNA splicing. Through profiling location Poly (ADP) ribose polymerase, we observed that it is associated at exon/intron boundaries genes, suggestive role for this enzyme alternative polymerase has previously been implicated PARylation splicing factors well modification H3K4me3, mark...
317 Background: ASKB589 is a humanized IgG1 monoclonal antibody against Claudin 18.2 (CLDN18.2) with high affinity and enhanced antibody-dependent cytotoxicity. We report preliminary safety efficacy data from an ongoing Phase Ib/II, dose-escalation expansion study of combined capecitabine, oxaliplatin(CAPOX) Sintilimab as first-line treatment G/GEJ adenocarcinoma (NCT05632939). Methods: The enrolled patients(pts) CLDN18.2 positive expression. phase used 3 + design to determine the maximum...
Using the cytoplasmic domain of insulin receptor (IR) in a yeast two-hybrid screen, we identified cDNA clone encoding C-terminal 308 amino acids human Stat5b (Stat5b-Ct). Stat5b-Ct is tyrosine phosphorylated by purified IR kinase vitro . Insulin stimulates phosphorylation overexpressed and endogenous Stat5 cells overexpressing IR. may be direct target and, as member Stat family transcription factors, play role regulation gene insulin. In support this hypothesis, perfusion mouse liver with...
BMS-813160 (compound 3) was identified as a potent and selective CCR2/5 dual antagonist. Compound 3 displayed good permeability at pH = 7.4 in PAMPA experiments demonstrated excellent human liver microsome stability. Pharmacokinetic studies established that had oral bioavailability exhibited low clearance dog cyno. also studied the mouse thioglycollate-induced peritonitis model, which confirmed its ability to inhibit migration of inflammatory monocytes macrophages. As result this profile,...
BackgroundNo standard maintenance treatment has been obtained to prolong the response duration of soft tissue sarcoma (STS) after first-line chemotherapy. In this study, we aimed evaluate efficacy and safety anlotinib as a chemotherapy in STS.MethodsIn multicentre, open-label, single-arm phase 2 trial, patients with advanced STS who achieved partial or stable disease anthracycline-based were enrolled between April 2019 January 2022. All received treatment. The primary endpoint was...
ATP-binding cassette transporters are ubiquitous in almost all organisms. The Escherichia coli genome is predicted to encode 69 ABC transporters. Eleven of the presumed be exporters, which seven possible drug export There has been minimal research on function YbhFSR, one putative resistance exporters. In this study, ybhF gene transporter was characterized. Overexpression and knockout strains were constructed. ATPase activity YbhF studied using malachite green assay, efflux abilities...
// Tao Li 1, * , Xiaoxia Liu 2, 3, Qin Shen 3 Wenjun Yang Zhenghao Huo Qilun 1 Haiyan Jiao Jing Chen Department of Oncology, General Hospital the Ningxia Medical University, Yinchuan 750004, China 2 Genetic and Cell Biology, Key Laboratory Fertility Preservation Maintenance (Ningxia University), Ministry Education, These authors contributed equally to this work Correspondence to: Chen, email: Chenjing1979@163.com Jiao, jiaohy65@163.com Keywords: gastric cancer, salinomycin, angiogenesis,...
Scaffold hopping and structure-based drug design were employed to identify substituted 4-aminoquinolines 4-aminonaphthyridines as potent, small molecule inhibitors of tumor necrosis factor alpha (TNFα). Structure–activity relationships in both the quinoline naphthyridine series leading identification compound 42 with excellent potency pharmacokinetic profile are discussed. X-ray co-crystal structure analysis ultracentrifugation experiments clearly demonstrate that these distort TNFα trimer...
We describe the hybridization of our previously reported acyclic and cyclic CC chemokine receptor 2 (CCR2) antagonists to lead a new series dual CCR2 CCR5. Installation γ-lactam as spacer group quinazoline benzamide mimetic improved oral bioavailability markedly. These efforts led identification 13d, potent orally bioavailable antagonist suitable for use in both murine monkey models inflammation.
Context: CYP3A4 and P-gp together form a highly efficient barrier for orally absorbed drugs always share the same substrates. Our previous work revealed that chrysosplenetin (CHR) significantly augmented rat plasma level anti-malarial efficacy of artemisinin (ART), partially due to uncompetitive inhibition effect CHR on CYP3A. But impact is still unknown.Objective: The present study investigates whether interferes with P-gp-mediated efflux ART elucidates underlying mechanism.Materials...
We encountered a dilemma in the course of studying series antagonists G-protein coupled receptor CC chemokine receptor-2 (CCR2): compounds with polar C3 side chains exhibited good ion channel selectivity but poor oral bioavailability, whereas lipophilic bioavailability preclinical species selectivity. Attempts to solve this through direct modulation physicochemical properties failed. However, installation protonation-dependent conformational switching mechanism resolved problem because it...
A series of novel, potent CCR1 inhibitors was developed from a moderately active hit using an iterative parallel synthesis approach. The initial (composed three subunits: amine, central amino acid, and N-terminal cap) became the basis for chemical libraries designed to generate SAR data. Libraries were synthesized that explored each subunits; binding data obtained revealed following: (1) changes amine are not well tolerated; (2) small alkylamino acids preferred in center molecule; (3)...