2-Phenoxy-nicotinamides are Potent Agonists at the Bile Acid Receptor GPBAR1 (TGR5)
Potency with potential: 2‐Phenoxy‐ nicotinamides were identified as potent agonists at the GPBAR1 receptor, a target in the treatment of obesity, type 2 diabetes and metabolic syndrome. Extensive structure–activity relationship studies supported by homology modeling and docking resulted in the ident...
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| Veröffentlicht in: | ChemMedChem 2013-04, Vol.8 (4), p.569-576 |
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| creator | Martin, Rainer E. Bissantz, Caterina Gavelle, Olivier Kuratli, Christoph Dehmlow, Henrietta Richter, Hans G. F. Obst Sander, Ulrike Erickson, Shawn D. Kim, Kyungjin Pietranico-Cole, Sherrie Lynn Alvarez-Sánchez, Rubén Ullmer, Christoph |
| description | Potency with potential: 2‐Phenoxy‐ nicotinamides were identified as potent agonists at the GPBAR1 receptor, a target in the treatment of obesity, type 2 diabetes and metabolic syndrome. Extensive structure–activity relationship studies supported by homology modeling and docking resulted in the identification of optimized GPBAR1 agonists, potent against both human and mouse receptors, endowed with favorable physicochemical properties and good metabolic stability. |
| doi_str_mv | 10.1002/cmdc.201200474 |
| format | Article |
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KGaA, Weinheim</rights><rights>Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.</rights><rights>Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4114-7f9e49c8ba92f08052bbefd169124c095b9e6b4a0bbffcbf66c5a31a5c009f663</citedby><cites>FETCH-LOGICAL-c4114-7f9e49c8ba92f08052bbefd169124c095b9e6b4a0bbffcbf66c5a31a5c009f663</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1002%2Fcmdc.201200474$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1002%2Fcmdc.201200474$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,776,780,1411,27901,27902,45550,45551</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/23225346$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Martin, Rainer E.</creatorcontrib><creatorcontrib>Bissantz, Caterina</creatorcontrib><creatorcontrib>Gavelle, Olivier</creatorcontrib><creatorcontrib>Kuratli, Christoph</creatorcontrib><creatorcontrib>Dehmlow, Henrietta</creatorcontrib><creatorcontrib>Richter, Hans G. 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| subjects | bile acid receptors Binding Sites GPBAR1 Humans metabolic disorders Molecular Docking Simulation Niacinamide - chemistry Niacinamide - metabolism nicotinamides Protein Binding Protein Structure, Tertiary Quinolines - chemistry Receptors, G-Protein-Coupled - agonists Receptors, G-Protein-Coupled - metabolism Structure-Activity Relationship structure-activity relationships |
| title | 2-Phenoxy-nicotinamides are Potent Agonists at the Bile Acid Receptor GPBAR1 (TGR5) |
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