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  • human glucagon receptor
  • We undertook a novel approach by generating high-affinity human monoclonal antibodies (mAbs) to the human glucagon receptor (GCGR) that display potent antagonistic activity in vitro and in vivo. (aspetjournals.org)
  • Beam me up: The new Nature study reports the crystal structure of the full-length human glucagon receptor (GCGR) that plays a key role in glucose homeostasis and serves as an important drug target for Type 2 diabetes. (cas.cn)
  • In addition to ASU, scientists at SIMM, in collaboration with several groups based in China (ShanghaiTech University, Zhengzhou University and Fudan University), United States (University of Southern California, The Scripps Research Institute, and GPCR Consortium), the Netherlands (Vrije Universiteit Amsterdam) and Denmark (Novo Nordisk), provided a detailed molecular map of the full-length human glucagon receptor (GCGR) in complex with a modulator (NNC0640) and the antigen-binding antibody fragment (mAb1). (cas.cn)
  • ligand
  • This may, in part, be due to technical difficulties associated with efficiently blocking the relatively large ligand/receptor-interacting pocket characteristic of the family B GPCRs. (aspetjournals.org)
  • PPARs regulate many metabolic pathways upon activation by endogenous ligands, such as fatty acids (FAs) and derivatives, or synthetic agonists, which bind to the ligand-binding domain of the receptor, triggering a conformational change. (jci.org)
  • PPARs are activated by FAs and their derivatives, and the level of physiologic receptor activation depends on the balance between ligand production and inactivation. (jci.org)
  • Particularly, the specific amino acid residues within the transmembrane helices and extracellular loops of the receptor that may confer ligand-induced receptor activation have been poorly investigated. (frontiersin.org)
  • However, the molecular mechanisms leading to high affinity ligand-receptor binding and receptor activation have not been fully understood. (frontiersin.org)
  • Receptor-ligand binding alters the conformation of the receptor and sends messages to the cell's interior, guiding cell function. (cas.cn)
  • Binding of a specific ligand to the glucagon receptor triggers the release of glucose from the liver during fasting, making this receptor a critical component for maintaining normal glucose levels in the body. (cas.cn)
  • retinoid X recept
  • 1,25D 3 binds to the vitamin D receptor (VDR), which forms a heterodimer with the retinoid X receptor and modulates gene expression. (diabetesjournals.org)
  • Subsequent recruitment of coactivators to the PPAR/retinoid X receptor heterodimer assembled at specific DNA response elements called PPAR response elements (PPREs) results in transactivation of target genes. (jci.org)
  • lipid
  • While they share anti-inflammatory activities, the PPAR isotypes distinguish themselves by differential actions on lipid and glucose homeostasis. (jci.org)
  • Glp1r
  • Despite the physiological and clinical importance of GLP-1, molecular interaction with the GLP-1 receptor (GLP1R) is not well understood. (frontiersin.org)
  • expression
  • D) Reagents and assays for the accurate expression and quantitation of functional incretin receptors in the endocrine/exocrine cells of the pancreas and relevant extrapancreatic tissues. (nih.gov)
  • The decreased expression of GLP-1R in the PVN and IFN of T2DM patients may be related to the dysregulation of feeding behavior and glucose homeostasis in T2DM. (uva.nl)
  • modulate
  • The increased calcium response mediated by secretin in the absence of GLP-1R was paralleled by an increased glucose-dependent insulin response, indicating that the heterodimeric receptor complexes modulate secretin responses. (nih.gov)
  • functional
  • It was further shown that glucagon-producing α-cells are topographically arranged for functional reasons with 91% of α-cells in the islets of Langerhans juxtaposed to β-cells. (diabetesjournals.org)
  • hypothalamus
  • In the hypothalamus, there are two types of appetite-regulating neurons: (a) coexpression of neuropeptide Y (NPY) and agouti-related protein (AgRP), both of which express melanocortin receptors (MCR) antagonists, and (b) proopiomelanocortin (POMC) which expresses MCR agonists [ 8 , 9 ]. (hindawi.com)