A5101983579- Receptor Mechanisms and Signaling
- Neuropeptides and Animal Physiology
- Computational Drug Discovery Methods
- Pregnancy-related medical research
- Diabetes Treatment and Management
- Bioinformatics and Genomic Networks
- Molecular Biology Techniques and Applications
- Hormonal Regulation and Hypertension
- Protein Structure and Dynamics
- Signaling Pathways in Disease
- RNA and protein synthesis mechanisms
- Estrogen and related hormone effects
- Adipose Tissue and Metabolism
- Advanced Drug Delivery Systems
- Pancreatic function and diabetes
- Chemical Synthesis and Analysis
- Fungal and yeast genetics research
- Biotin and Related Studies
- Drug Solubulity and Delivery Systems
- Steroid Chemistry and Biochemistry
- Advanced Biosensing Techniques and Applications
- Prostate Cancer Treatment and Research
- Monoclonal and Polyclonal Antibodies Research
- bioluminescence and chemiluminescence research
- Drug-Induced Hepatotoxicity and Protection
University of Science and Technology of China
2024
National Center for Drug Screening
2008-2020
Shanghai Institute of Materia Medica
2008-2020
University of Chinese Academy of Sciences
2017-2019
Chinese Academy of Sciences
2014
Abstract Accurate identification of compound–protein interactions (CPIs) in silico may deepen our understanding the underlying mechanisms drug action and thus remarkably facilitate discovery development. Conventional similarity- or docking-based computational methods for predicting CPIs rarely exploit latent features from currently available large-scale unlabeled compound protein data often limit their usage to relatively small-scale datasets. In present study, we propose DeepCPI, a novel...
Insulin-like peptide 5 (INSL5), a member of the insulin/relaxin superfamily, can activate G-protein-coupled receptor relaxin/insulin-like family 4 (RXFP4), but its precise biological functions are largely unknown. Recent studies suggest that INSL5/RXFP4 is involved in control food intake and glucose homoeostasis. We report present study RXFP4 mouse insulinoma cell line MIN6 INSL5 augments glucose-stimulated insulin secretion (GSIS) both vitro vivo. also expressed intestinal L-cell GLUTag...
The calcitonin receptor (CTR) is a class B G protein-coupled (GPCR) that responds to the peptide hormone (CT). CTs are clinically approved for treatment of bone diseases. We previously reported 4.1 Å structure activated CTR bound salmon CT (sCT) and heterotrimeric Gs protein by cryo-electron microscopy (Liang, Y.-L., et al. Phase-plate cryo- EM GPCR-G complex. Nature 2017, 546, 118–123). In current study, we have reprocessed electron micrographs yield 3.3 map This has allowed us model...
Class B peptide hormone GPCRs are targets for the treatment of major chronic disease. Peptide ligands these receptors display biased agonism and this may provide future therapeutic advantage. Recent active structures calcitonin (CT) glucagon-like peptide-1 (GLP-1) reveal distinct engagement peptides with extracellular loops (ECLs) 2 3, mutagenesis GLP-1R has implicated in dynamics receptor activation. In current study, we have mutated ECLs 3 human CT (CTR), to interrogate expression,...
Selective androgen receptor modulators are of great value in the treatment prostate cancer. The purpose this study was to provide a preliminary characterization new class non-steroidal discovered high-throughput screening campaign.Competitive binding, luciferase-based reporter methods, cell proliferation and vivo assays were employed evaluate an initial set compounds from chemistry efforts.Forty-nine analogues efforts showed high affinity binding receptors, agonist and/or antagonist...
Amylin is coexpressed with insulin in pancreatic islet β-cells and has potent effects on gastric emptying food intake. The effect of amylin satiation been postulated to involve AMY3 receptors (AMY3R) that are heteromers the calcitonin receptor (CTR) activity-modifying protein 3 (RAMP3). Understanding molecular control signaling through AMY3R thus important for peptide drug targeting this receptor. We have previously used alanine scanning mutagenesis study contribution extracellular surface...
GLP-1R (glucagon-like peptide-1 receptor) mediates the 'incretin effect' and many other anti-diabetic actions of its cognate ligand, GLP-1 peptide-1). It belongs to class B family GPCRs (G protein-coupled receptors) possesses an N-terminal putative SP (signal peptide). has been reported that this sequence is required for synthesis cleaved after receptor synthesis. In present study, we conducted in-depth exploration towards role in A mutant without was expressed HEK293 cells (human embryonic...