Matches in SemOpenAlex for { <https://semopenalex.org/work/W4309079919> ?p ?o ?g. }
- W4309079919 endingPage "114927" @default.
- W4309079919 startingPage "114927" @default.
- W4309079919 abstract "Adiponectin and leptin are major adipocytokines that control crosstalk between adipose tissue and other organ systems. Hypoadiponectinemia and hypoleptinemia are associated with human metabolic diseases. Compounds with adipocytokine biosynthesis-stimulating activities could be developed as therapeutics against diverse metabolic conditions. In phenotypic screening with human bone marrow mesenchymal stem cells (hBM-MSCs), (E)-4-hydroxy-3-(3-(4-hydroxy-3-methoxyphenyl)acryloyl)-6-methyl-2H-pyran-2-one (1) was identified to increase adiponectin biosynthesis during adipogenesis and simultaneously to stimulate leptin production. Using the compound 1 structure, the structure-activity relationship study was performed to discover more potent compounds stimulating both adiponectin and leptin production. (E)-3-(3-(2-fluoropyridin-4-yl)acryloyl)-4-hydroxy-6-methyl-2H-pyran-2-one (11) exhibited the most potent adiponectin (EC50, 2.87 μM) and leptin (EC50, 2.82 μM) biosynthesis-stimulating activities in hBM-MSCs. In a target identification study, compound 11 was characterized as a dual modulator binding to both peroxisome proliferator-activated receptor (PPAR) γ and glucocorticoid receptor (GR). This study provides a novel pharmacophore for PPARγ/GR dual modulators with therapeutic potential against human metabolic diseases." @default.
- W4309079919 created "2022-11-21" @default.
- W4309079919 creator A5004975261 @default.
- W4309079919 creator A5015662258 @default.
- W4309079919 creator A5018771950 @default.
- W4309079919 creator A5018847566 @default.
- W4309079919 creator A5023107984 @default.
- W4309079919 creator A5043666983 @default.
- W4309079919 creator A5053003028 @default.
- W4309079919 creator A5067527102 @default.
- W4309079919 creator A5067974244 @default.
- W4309079919 creator A5072899204 @default.
- W4309079919 creator A5076094908 @default.
- W4309079919 creator A5078463338 @default.
- W4309079919 creator A5079570948 @default.
- W4309079919 date "2023-01-01" @default.
- W4309079919 modified "2023-10-02" @default.
- W4309079919 title "Discovery of PPARγ and glucocorticoid receptor dual agonists to promote the adiponectin and leptin biosynthesis in human bone marrow mesenchymal stem cells" @default.
- W4309079919 cites W1971252291 @default.
- W4309079919 cites W1980089744 @default.
- W4309079919 cites W1980143981 @default.
- W4309079919 cites W1989994069 @default.
- W4309079919 cites W1995292479 @default.
- W4309079919 cites W1995378042 @default.
- W4309079919 cites W2008768221 @default.
- W4309079919 cites W2020536236 @default.
- W4309079919 cites W2053073979 @default.
- W4309079919 cites W2059109343 @default.
- W4309079919 cites W2059358536 @default.
- W4309079919 cites W2060292857 @default.
- W4309079919 cites W2068837005 @default.
- W4309079919 cites W2077539293 @default.
- W4309079919 cites W2079105050 @default.
- W4309079919 cites W2087613795 @default.
- W4309079919 cites W2113456624 @default.
- W4309079919 cites W2119963782 @default.
- W4309079919 cites W2125539316 @default.
- W4309079919 cites W2135009079 @default.
- W4309079919 cites W2139031643 @default.
- W4309079919 cites W2147627625 @default.
- W4309079919 cites W2155036285 @default.
- W4309079919 cites W2158330544 @default.
- W4309079919 cites W2163226222 @default.
- W4309079919 cites W2225259556 @default.
- W4309079919 cites W2330751715 @default.
- W4309079919 cites W2345537052 @default.
- W4309079919 cites W2361659253 @default.
- W4309079919 cites W2415267894 @default.
- W4309079919 cites W2475311184 @default.
- W4309079919 cites W2519479884 @default.
- W4309079919 cites W2568322374 @default.
- W4309079919 cites W2596585859 @default.
- W4309079919 cites W2744291240 @default.
- W4309079919 cites W2769161407 @default.
- W4309079919 cites W2777479722 @default.
- W4309079919 cites W2781240994 @default.
- W4309079919 cites W2787494000 @default.
- W4309079919 cites W2789238930 @default.
- W4309079919 cites W2912431762 @default.
- W4309079919 cites W2920830318 @default.
- W4309079919 cites W2942002737 @default.
- W4309079919 cites W2944905560 @default.
- W4309079919 cites W2978687867 @default.
- W4309079919 cites W2994733157 @default.
- W4309079919 cites W3006060321 @default.
- W4309079919 cites W3009267861 @default.
- W4309079919 cites W3017310129 @default.
- W4309079919 cites W3037518248 @default.
- W4309079919 cites W3136548257 @default.
- W4309079919 cites W3165732199 @default.
- W4309079919 cites W4221129331 @default.
- W4309079919 cites W4284890877 @default.
- W4309079919 doi "https://doi.org/10.1016/j.ejmech.2022.114927" @default.
- W4309079919 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36379105" @default.
- W4309079919 hasPublicationYear "2023" @default.
- W4309079919 type Work @default.
- W4309079919 citedByCount "3" @default.
- W4309079919 countsByYear W43090799192022 @default.
- W4309079919 countsByYear W43090799192023 @default.
- W4309079919 crossrefType "journal-article" @default.
- W4309079919 hasAuthorship W4309079919A5004975261 @default.
- W4309079919 hasAuthorship W4309079919A5015662258 @default.
- W4309079919 hasAuthorship W4309079919A5018771950 @default.
- W4309079919 hasAuthorship W4309079919A5018847566 @default.
- W4309079919 hasAuthorship W4309079919A5023107984 @default.
- W4309079919 hasAuthorship W4309079919A5043666983 @default.
- W4309079919 hasAuthorship W4309079919A5053003028 @default.
- W4309079919 hasAuthorship W4309079919A5067527102 @default.
- W4309079919 hasAuthorship W4309079919A5067974244 @default.
- W4309079919 hasAuthorship W4309079919A5072899204 @default.
- W4309079919 hasAuthorship W4309079919A5076094908 @default.
- W4309079919 hasAuthorship W4309079919A5078463338 @default.
- W4309079919 hasAuthorship W4309079919A5079570948 @default.
- W4309079919 hasConcept C122927707 @default.
- W4309079919 hasConcept C126322002 @default.
- W4309079919 hasConcept C134018914 @default.
- W4309079919 hasConcept C14372207 @default.
- W4309079919 hasConcept C171089720 @default.