Matches in SemOpenAlex for { <https://semopenalex.org/work/W2606222255> ?p ?o ?g. }
- W2606222255 endingPage "4211" @default.
- W2606222255 startingPage "4185" @default.
- W2606222255 abstract "The role of the G-protein-coupled bile acid receptor TGR5 in various organs, tissues, and cell types, specifically in intestinal endocrine L-cells and brown adipose tissue, has made it a promising therapeutical target in several diseases, especially type-2 diabetes and metabolic syndrome. However, recent studies have shown deleterious on-target effects of systemic TGR5 agonists. To avoid these systemic effects while stimulating glucagon-like peptide-1 (GLP-1) secreting enteroendocrine L-cells, we have designed TGR5 agonists with low intestinal permeability. In this article, we describe their synthesis, characterization, and biological evaluation. Among them, compound 24 is a potent GLP-1 secretagogue, has low effect on gallbladder volume, and improves glucose homeostasis in a preclinical murine model of diet-induced obesity and insulin resistance, making the proof of concept of the potential of topical intestinal TGR5 agonists as therapeutic agents in type-2 diabetes." @default.
- W2606222255 created "2017-04-28" @default.
- W2606222255 creator A5001127450 @default.
- W2606222255 creator A5003139544 @default.
- W2606222255 creator A5007648204 @default.
- W2606222255 creator A5013140552 @default.
- W2606222255 creator A5016801110 @default.
- W2606222255 creator A5023719156 @default.
- W2606222255 creator A5024558218 @default.
- W2606222255 creator A5025657305 @default.
- W2606222255 creator A5027322365 @default.
- W2606222255 creator A5032258154 @default.
- W2606222255 creator A5046200375 @default.
- W2606222255 creator A5051979702 @default.
- W2606222255 creator A5062340044 @default.
- W2606222255 creator A5071070119 @default.
- W2606222255 creator A5071290936 @default.
- W2606222255 creator A5074853395 @default.
- W2606222255 creator A5075797064 @default.
- W2606222255 creator A5088966082 @default.
- W2606222255 creator A5090653750 @default.
- W2606222255 date "2017-05-05" @default.
- W2606222255 modified "2023-10-18" @default.
- W2606222255 title "Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance" @default.
- W2606222255 cites W1489601464 @default.
- W2606222255 cites W1895112498 @default.
- W2606222255 cites W1911520061 @default.
- W2606222255 cites W1963587340 @default.
- W2606222255 cites W1965796890 @default.
- W2606222255 cites W1967442749 @default.
- W2606222255 cites W2000210192 @default.
- W2606222255 cites W2011505858 @default.
- W2606222255 cites W2028990131 @default.
- W2606222255 cites W2043759658 @default.
- W2606222255 cites W2053833972 @default.
- W2606222255 cites W2068049423 @default.
- W2606222255 cites W2081028309 @default.
- W2606222255 cites W2088762974 @default.
- W2606222255 cites W2096418655 @default.
- W2606222255 cites W2103797163 @default.
- W2606222255 cites W2105649494 @default.
- W2606222255 cites W2111157610 @default.
- W2606222255 cites W2113961306 @default.
- W2606222255 cites W2121911364 @default.
- W2606222255 cites W2146764867 @default.
- W2606222255 cites W2157101557 @default.
- W2606222255 cites W2158609797 @default.
- W2606222255 cites W2315996040 @default.
- W2606222255 cites W2464084730 @default.
- W2606222255 cites W2950166688 @default.
- W2606222255 doi "https://doi.org/10.1021/acs.jmedchem.6b01873" @default.
- W2606222255 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/28414465" @default.
- W2606222255 hasPublicationYear "2017" @default.
- W2606222255 type Work @default.
- W2606222255 sameAs 2606222255 @default.
- W2606222255 citedByCount "47" @default.
- W2606222255 countsByYear W26062222552018 @default.
- W2606222255 countsByYear W26062222552019 @default.
- W2606222255 countsByYear W26062222552020 @default.
- W2606222255 countsByYear W26062222552021 @default.
- W2606222255 countsByYear W26062222552022 @default.
- W2606222255 countsByYear W26062222552023 @default.
- W2606222255 crossrefType "journal-article" @default.
- W2606222255 hasAuthorship W2606222255A5001127450 @default.
- W2606222255 hasAuthorship W2606222255A5003139544 @default.
- W2606222255 hasAuthorship W2606222255A5007648204 @default.
- W2606222255 hasAuthorship W2606222255A5013140552 @default.
- W2606222255 hasAuthorship W2606222255A5016801110 @default.
- W2606222255 hasAuthorship W2606222255A5023719156 @default.
- W2606222255 hasAuthorship W2606222255A5024558218 @default.
- W2606222255 hasAuthorship W2606222255A5025657305 @default.
- W2606222255 hasAuthorship W2606222255A5027322365 @default.
- W2606222255 hasAuthorship W2606222255A5032258154 @default.
- W2606222255 hasAuthorship W2606222255A5046200375 @default.
- W2606222255 hasAuthorship W2606222255A5051979702 @default.
- W2606222255 hasAuthorship W2606222255A5062340044 @default.
- W2606222255 hasAuthorship W2606222255A5071070119 @default.
- W2606222255 hasAuthorship W2606222255A5071290936 @default.
- W2606222255 hasAuthorship W2606222255A5074853395 @default.
- W2606222255 hasAuthorship W2606222255A5075797064 @default.
- W2606222255 hasAuthorship W2606222255A5088966082 @default.
- W2606222255 hasAuthorship W2606222255A5090653750 @default.
- W2606222255 hasBestOaLocation W26062222552 @default.
- W2606222255 hasConcept C103395026 @default.
- W2606222255 hasConcept C126322002 @default.
- W2606222255 hasConcept C134018914 @default.
- W2606222255 hasConcept C170493617 @default.
- W2606222255 hasConcept C185592680 @default.
- W2606222255 hasConcept C2776398474 @default.
- W2606222255 hasConcept C2777180221 @default.
- W2606222255 hasConcept C2777391703 @default.
- W2606222255 hasConcept C2779306644 @default.
- W2606222255 hasConcept C2779399885 @default.
- W2606222255 hasConcept C2780161494 @default.
- W2606222255 hasConcept C2781071285 @default.
- W2606222255 hasConcept C3018667095 @default.
- W2606222255 hasConcept C39321552 @default.
- W2606222255 hasConcept C46699223 @default.