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  • agonists
  • Therefore, orally active small-molecule agonists or modulators that augment signaling via the GLP-1 receptor are highly desirable. (aspetjournals.org)
  • This was exemplified by the thiazolidinediones, nuclear receptor agonists with useful glucose-lowering properties but pleiotropic and unpredictable pathophysiological actions. (diabetesjournals.org)
  • The present invention relates to the medical use of specific GLP-1 /glucagon receptor agonists in the prevention and/or treatment of metabolic liver disease, particularly non-alcoholic fatty liver disease (NAFLD), more particularly non-alcoholic fatty liver (NAFL), non-alcoholic steatohepatitis (NASH) and/or NAFLD-associated liver fibrosis. (wipo.int)
  • membrane
  • Because the receptor is the first in its class of membrane proteins to be structurally determined, the work may advance studies of similarly shaped, medically important but often difficult to characterize molecules. (scripps.edu)
  • These receptors are very different from the class A receptors since they have key functional domains both embedded in and outside of the cellular membrane, so the lessons we've learned from the class A have not been entirely applicable," said Vsevolod Katritch, an assistant professor of molecular biology at TSRI and a co-author on the study. (scripps.edu)
  • X-ray crystallography yields the complete, detailed, architecture of this class B membrane protein receptor for the first time, dramatically improving the prospects for a new generation of highly specific drugs for treating Type 2 diabetes with greater effectiveness and fewer side effects. (cas.cn)
  • novel
  • Characterization of three corticotropin-releasing factor receptors in catfish: a novel third receptor is predominantly expressed in pituitary and urophysis. (embl-heidelberg.de)
  • This novel CRF receptor (cfCRF-R3) bound CRF with a 5-fold higher affinity than urotensin I and sauvagine and was expressed in the pituitary gland, urophysis, and brain. (embl-heidelberg.de)
  • Exendin-4 is now employed in humans as a novel therapy for diabetes. (bmj.com)
  • GLP1
  • The pre-coated antibody is human GLP1 monoclonal antibody and the detecting antibody is polyclonal antibody with biotin labeled. (mybiosource.com)
  • rats
  • Although the predominant transgenic host species has been mouse, the genomes of rats, rabbits, chickens, and cows have also been modified to express human antibodies. (frontiersin.org)
  • specificity
  • Such information is vital for the development of effective drugs, which must bind with their complex target cell receptors with great specificity. (cas.cn)
  • proteins
  • Over the past decade, the Stevens and Cherezov laboratories at TSRI have pioneered techniques to express, stabilize and induce these inherently flexible receptor proteins to form regular crystalline solids-from which their structures can be derived using a technique called X-ray crystallography. (scripps.edu)
  • antibodies
  • Therapeutic molecules derived from antibodies have become a dominant class of drugs used to treat human disease. (frontiersin.org)
  • Increasingly, therapeutic antibodies are discovered using transgenic animal systems that have been engineered to express human antibodies. (frontiersin.org)
  • While the engineering details differ, these platforms share the ability to raise an immune response that is comprised of antibodies with fully human idiotypes. (frontiersin.org)
  • Affinity
  • Ideal antibody candidates are often required to bind with high affinity to a specific epitope, cross-react to a non-human ortholog, lack binding to paralogs, and survive the rigors of the stringent drug development process ( 6 ). (frontiersin.org)
  • diabetes
  • The hope was that these new cells might be able to replace those that died off in the course of human diabetes. (bmj.com)
  • Interferon-gamma receptor signaling is dispensable in the development of autoimmune type 1 diabetes in NOD mice. (diabetesjournals.org)
  • Their findings shed new light on the structure of the glucagon receptor, a highly promising target for diabetes drug development. (cas.cn)
  • Pharmaceutical companies hope to develop new drugs that can more accurately and efficiently bind with cell receptors, including diabetes drugs that will be able to halt or reduce the overproduction of glucose. (cas.cn)
  • expression
  • Anatomical profiling of G protein-coupled receptor expression. (guidetopharmacology.org)
  • However, a detailed description of GLP-1R expression in the human hypothalamus is lacking, and it is unknown whether this expression is altered in T2DM patients. (uva.nl)
  • The objective of the study was to investigate the GLP-1R distribution in the human postmortem hypothalamus and to determine whether hypothalamic GLP-1R expression is altered in T2DM patients. (uva.nl)
  • We investigated the distribution of GLP-1R expression throughout the human hypothalamus by means of in situ hybridization. (uva.nl)
  • molecules
  • The results of the new study are significant because all three parts of the receptor are essential for its ability to properly bind with its target molecules. (cas.cn)