Matches in SemOpenAlex for { <https://semopenalex.org/work/W3022198561> ?p ?o ?g. }
- W3022198561 endingPage "1534" @default.
- W3022198561 startingPage "1526" @default.
- W3022198561 abstract "A known natural product, magnaldehyde B, was identified as an agonist of retinoid X receptor (RXR) α. Magnaldehyde B was isolated from Magnolia obovata (Magnoliaceae) and synthesized along with more potent analogs for screening of their RXRα agonistic activities. Structural optimization of magnaldehyde B resulted in the development of a candidate molecule that displayed a 440-fold increase in potency. Receptor-ligand docking simulations indicated that this molecule has the highest affinity with the ligand binding domain of RXRα among the analogs synthesized in this study. Furthermore, the selective activation of the peroxisome proliferator-activated receptor (PPAR) δ-RXR heterodimer with a stronger efficacy compared to those of PPARα-RXR and PPARγ-RXR was achieved in luciferase reporter assays using the PPAR response element driven reporter (PPRE-Luc). The PPARδ activity of the molecule was significantly inhibited by the antagonists of both RXR and PPARδ, whereas the activity of GW501516 was not affected by the RXR antagonist. Furthermore, the molecule exhibited a particularly weak PPARδ agonistic activity in reporter gene assays using the Gal4 hybrid system. The obtained data therefore suggest that the weak PPARδ agonistic activity of the optimized molecule is synergistically enhanced by its own RXR agonistic activity, indicating the potent agonistic activity of the PPARδ-RXR heterodimer." @default.
- W3022198561 created "2020-05-13" @default.
- W3022198561 creator A5010975602 @default.
- W3022198561 creator A5017473881 @default.
- W3022198561 creator A5018941611 @default.
- W3022198561 creator A5049020167 @default.
- W3022198561 creator A5053435376 @default.
- W3022198561 creator A5066382334 @default.
- W3022198561 creator A5069596286 @default.
- W3022198561 creator A5072125235 @default.
- W3022198561 creator A5077654395 @default.
- W3022198561 creator A5082991123 @default.
- W3022198561 creator A5085766889 @default.
- W3022198561 date "2020-05-06" @default.
- W3022198561 modified "2023-09-23" @default.
- W3022198561 title "Discovery and SAR of Natural-Product-Inspired RXR Agonists with Heterodimer Selectivity to PPARδ-RXR" @default.
- W3022198561 cites W1127276322 @default.
- W3022198561 cites W1596796792 @default.
- W3022198561 cites W1980222251 @default.
- W3022198561 cites W2004811381 @default.
- W3022198561 cites W2017149825 @default.
- W3022198561 cites W2036247576 @default.
- W3022198561 cites W2040053707 @default.
- W3022198561 cites W2059109343 @default.
- W3022198561 cites W2065886331 @default.
- W3022198561 cites W2079266078 @default.
- W3022198561 cites W2079921490 @default.
- W3022198561 cites W2081388499 @default.
- W3022198561 cites W2084088632 @default.
- W3022198561 cites W2091544680 @default.
- W3022198561 cites W2096639035 @default.
- W3022198561 cites W2096705448 @default.
- W3022198561 cites W2106371119 @default.
- W3022198561 cites W2112614409 @default.
- W3022198561 cites W2115229208 @default.
- W3022198561 cites W2127550817 @default.
- W3022198561 cites W2134967712 @default.
- W3022198561 cites W2141662437 @default.
- W3022198561 cites W2151807579 @default.
- W3022198561 cites W2166156558 @default.
- W3022198561 cites W2170969811 @default.
- W3022198561 cites W2171824864 @default.
- W3022198561 cites W2302434278 @default.
- W3022198561 cites W2325067113 @default.
- W3022198561 cites W2519479884 @default.
- W3022198561 cites W2605614532 @default.
- W3022198561 cites W2611398367 @default.
- W3022198561 cites W2735052425 @default.
- W3022198561 cites W2766894047 @default.
- W3022198561 cites W2792659208 @default.
- W3022198561 cites W2793564315 @default.
- W3022198561 cites W2794794281 @default.
- W3022198561 cites W2891657250 @default.
- W3022198561 cites W2914645254 @default.
- W3022198561 cites W4206932187 @default.
- W3022198561 cites W2461630679 @default.
- W3022198561 doi "https://doi.org/10.1021/acschembio.0c00146" @default.
- W3022198561 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32374156" @default.
- W3022198561 hasPublicationYear "2020" @default.
- W3022198561 type Work @default.
- W3022198561 sameAs 3022198561 @default.
- W3022198561 citedByCount "4" @default.
- W3022198561 countsByYear W30221985612020 @default.
- W3022198561 countsByYear W30221985612022 @default.
- W3022198561 countsByYear W30221985612023 @default.
- W3022198561 crossrefType "journal-article" @default.
- W3022198561 hasAuthorship W3022198561A5010975602 @default.
- W3022198561 hasAuthorship W3022198561A5017473881 @default.
- W3022198561 hasAuthorship W3022198561A5018941611 @default.
- W3022198561 hasAuthorship W3022198561A5049020167 @default.
- W3022198561 hasAuthorship W3022198561A5053435376 @default.
- W3022198561 hasAuthorship W3022198561A5066382334 @default.
- W3022198561 hasAuthorship W3022198561A5069596286 @default.
- W3022198561 hasAuthorship W3022198561A5072125235 @default.
- W3022198561 hasAuthorship W3022198561A5077654395 @default.
- W3022198561 hasAuthorship W3022198561A5082991123 @default.
- W3022198561 hasAuthorship W3022198561A5085766889 @default.
- W3022198561 hasConcept C104317684 @default.
- W3022198561 hasConcept C118792377 @default.
- W3022198561 hasConcept C128821507 @default.
- W3022198561 hasConcept C161790260 @default.
- W3022198561 hasConcept C170493617 @default.
- W3022198561 hasConcept C185592680 @default.
- W3022198561 hasConcept C187345961 @default.
- W3022198561 hasConcept C21951064 @default.
- W3022198561 hasConcept C2779396153 @default.
- W3022198561 hasConcept C55493867 @default.
- W3022198561 hasConcept C63932345 @default.
- W3022198561 hasConcept C71240020 @default.
- W3022198561 hasConcept C86339819 @default.
- W3022198561 hasConcept C86803240 @default.
- W3022198561 hasConcept C95444343 @default.
- W3022198561 hasConceptScore W3022198561C104317684 @default.
- W3022198561 hasConceptScore W3022198561C118792377 @default.
- W3022198561 hasConceptScore W3022198561C128821507 @default.
- W3022198561 hasConceptScore W3022198561C161790260 @default.
- W3022198561 hasConceptScore W3022198561C170493617 @default.
- W3022198561 hasConceptScore W3022198561C185592680 @default.