Results 51 to 60 of about 11,220 (181)
The G protein–coupled receptor (GPCR) superfamily consists of the most common targets of approved drugs. Targeting GPCRs offers appealing avenues for therapeutic development. Antibodies and their fragments, such as single‐domain antibodies (VHHs or nanobodies), have emerged as useful alternatives to small molecule pharmacophores as building blocks in ...
Shivani Sachdev, Ross W. Cheloha
wiley +1 more source
The role of opioid peptides in the regulation of secretin-stimulated bile secretion
Influence of intraperitoneal dalargin (dand m-opioid agonist), DADLE (d-opioid agonist), DAGO (m-opioid agonist) and U50488 (k-opioid agonist) on bile secretion which is stimulated by secretin was studied in sharp experiments on white rats.
M. A. Medvedev, I. V. Roudin
doaj +1 more source
GIP in Cardiovascular and Kidney Disease: From Physiology to Pharmacology
ABSTRACT Aims To provide a comprehensive overview of the cardiovascular and renal effects of glucose‐dependent insulinotropic polypeptide (GIP) by integrating its physiological role with recent human trial data on tirzepatide, the first dual GIP and glucagon‐like peptide‐1 (GLP‐1) receptor agonist.
Michelantonio De Fano +4 more
wiley +1 more source
Impact of secretin receptor homo-dimerization on natural ligand binding
Class B G protein-coupled receptors can form dimeric complexes important for high potency biological effects. Here, we apply pharmacological, biochemical, and biophysical techniques to cells and membranes expressing the prototypic secretin receptor (SecR)
Kaleeckal G. Harikumar +5 more
doaj +1 more source
ABSTRACT Background and Aims Malnutrition disorders are associated with an enteropathy characterized by villus blunting, secretory cell loss, and mucosal inflammation. To investigate the contribution of undernutrition to enteropathy we conducted a case–control study of adult patients with starvation due to benign esophageal strictures, compared with ...
Ellen Besa +7 more
wiley +1 more source
The type II secretion system (T2SS) releases large folded exoproteins across the envelope of many Gram-negative pathogens. This secretion process therefore requires specific gating, interacting, and dynamics properties mainly operated by a bipartite ...
Badreddine Douzi +11 more
doaj +1 more source
Interplay of the ENS and Microbiota With Murine Gut Epithelium‐Derived Organoids in Aging
A gut organoid model was developed to study the impact of age‐related changes of the enteric nervous system (ENS) and microbiome on the integrity and trophic capacity of the intestinal epithelial barrier. Organoids reflected in vivo aging features, including altered epithelial integrity and changes in acetylcholine‐related enzyme activity.
Tinh Thi Nguyen +12 more
wiley +1 more source
Abstract Background A drug designed for a specific target often interacts with multiple targets, either unintentionally or as part of its intended mechanism of action. This has been called pharmacological pleiotropy or polypharmacology. There are key endogenous ligands such as ATP, GABA and glutamate that act on various proteins in humans. Furthermore,
Hampus Ljunggren +8 more
wiley +1 more source
GPCRs in CAR‐T Cell Immunotherapy: Expanding the Target Landscape and Enhancing Therapeutic Efficacy
Chimeric antigen receptor T cell therapy faces dual challenges of target scarcity and an immunosuppressive microenvironment in solid tumors. This review highlights how G protein‐coupled receptors can serve as both novel targets to expand the therapeutic scope and functional modules to enhance CAR‐T cell efficacy.
Zhuoqun Liu +11 more
wiley +1 more source
Advances in GPCRs Associated With Wnt Signaling Within the Auditory System
ABSTRACT G protein‐coupled receptors (GPCRs) that interact with the Wnt signaling pathway are pivotal for auditory system homeostasis, as they orchestrate inner ear development, hair cell (HC) regeneration, and hearing preservation. Frizzled (FZD) receptors, the core Wnt‐related GPCRs, bind Wnt ligands and co‐receptors (e.g., LRP5/6) to activate both ...
Liang Wang +3 more
wiley +1 more source

