FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2887375268> ?p ?o ?g. }

• W2887375268 endingPage "178" @default.
• W2887375268 startingPage "169" @default.
• W2887375268 abstract "11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) is a cortisol regenerating enzyme that amplifies tissue glucocorticoid levels, especially in the liver and adipose tissue. Knockout mice or a selective inhibitor of 11β-HSD1 improves metabolic syndrome parameters in preclinical models and human clinical trials. Here, we evaluated the therapeutic potential of INU-101, a potent and selective oral inhibitor of 11β-HSD1. The in vitro activity of 11β-HSD1 was measured using the homogeneous time-resolved fluorescence (HTRF) assay. Differentiated adipocytes were used to evaluate the cellular 11β-HSD1 activity. To determine the inhibitory effects on 11β-HSD1 in tissues, we performed ex vivo studies using liver and adipose tissue isolated from C57BL/6 J mice and Cynomolgus monkeys. KKAy mice, ob/ob mice and ZDF rats were administered INU-101 to evaluate whether this compound ameliorated metabolic abnormalities in obese and diabetic animals. INU-101 had highly potent inhibitory activity in mouse, monkey and human 11β-HSD1, derived from liver microsomes. The oral administration of INU-101 significantly inhibited 11β-HSD1 activity in the liver and adipose tissue of mice and monkeys. In KKAy mice, ob/ob mice and ZDF rats, the oral administration of INU-101 enhanced insulin sensitivity and lowered the fasting blood glucose level. Furthermore, INU-101 treatment decreased the body weight and ameliorated an improved lipid profile in the diabetic mouse model. These results suggest that the 11β-HSD1 inhibitor, INU-101 may serve as a novel drug candidate for the treatment of type 2 diabetes and metabolic syndrome." @default.
• W2887375268 created "2018-08-22" @default.
• W2887375268 creator A5004975261 @default.
• W2887375268 creator A5047657361 @default.
• W2887375268 creator A5081021239 @default.
• W2887375268 creator A5088267834 @default.
• W2887375268 date "2018-09-01" @default.
• W2887375268 modified "2023-09-23" @default.
• W2887375268 title "A novel highly potent and selective 11β-hydroxysteroid dehydrogenase type 1 inhibitor, INU-101" @default.
• W2887375268 cites W1610975395 @default.
• W2887375268 cites W1965576057 @default.
• W2887375268 cites W1973619189 @default.
• W2887375268 cites W1975045088 @default.
• W2887375268 cites W1976973182 @default.
• W2887375268 cites W1978998045 @default.
• W2887375268 cites W1981847955 @default.
• W2887375268 cites W1985540243 @default.
• W2887375268 cites W1999174748 @default.
• W2887375268 cites W2042293558 @default.
• W2887375268 cites W2042443117 @default.
• W2887375268 cites W2052586752 @default.
• W2887375268 cites W2052787253 @default.
• W2887375268 cites W2086635975 @default.
• W2887375268 cites W2092020543 @default.
• W2887375268 cites W2100159933 @default.
• W2887375268 cites W2117268230 @default.
• W2887375268 cites W2119251936 @default.
• W2887375268 cites W2127017620 @default.
• W2887375268 cites W2136064817 @default.
• W2887375268 cites W2152760742 @default.
• W2887375268 cites W2153965794 @default.
• W2887375268 cites W2154972651 @default.
• W2887375268 cites W2156597872 @default.
• W2887375268 cites W753142686 @default.
• W2887375268 doi "https://doi.org/10.1016/j.ejphar.2018.08.005" @default.
• W2887375268 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30096297" @default.
• W2887375268 hasPublicationYear "2018" @default.
• W2887375268 type Work @default.
• W2887375268 sameAs 2887375268 @default.
• W2887375268 citedByCount "6" @default.
• W2887375268 countsByYear W28873752682020 @default.
• W2887375268 countsByYear W28873752682021 @default.
• W2887375268 countsByYear W28873752682023 @default.
• W2887375268 crossrefType "journal-article" @default.
• W2887375268 hasAuthorship W2887375268A5004975261 @default.
• W2887375268 hasAuthorship W2887375268A5047657361 @default.
• W2887375268 hasAuthorship W2887375268A5081021239 @default.
• W2887375268 hasAuthorship W2887375268A5088267834 @default.
• W2887375268 hasConcept C126322002 @default.
• W2887375268 hasConcept C134018914 @default.
• W2887375268 hasConcept C150903083 @default.
• W2887375268 hasConcept C166075782 @default.
• W2887375268 hasConcept C171089720 @default.
• W2887375268 hasConcept C181199279 @default.
• W2887375268 hasConcept C185592680 @default.
• W2887375268 hasConcept C207001950 @default.
• W2887375268 hasConcept C2776317432 @default.
• W2887375268 hasConcept C2777056448 @default.
• W2887375268 hasConcept C2777180221 @default.
• W2887375268 hasConcept C2780578515 @default.
• W2887375268 hasConcept C2780841215 @default.
• W2887375268 hasConcept C55493867 @default.
• W2887375268 hasConcept C555293320 @default.
• W2887375268 hasConcept C71924100 @default.
• W2887375268 hasConcept C86803240 @default.
• W2887375268 hasConceptScore W2887375268C126322002 @default.
• W2887375268 hasConceptScore W2887375268C134018914 @default.
• W2887375268 hasConceptScore W2887375268C150903083 @default.
• W2887375268 hasConceptScore W2887375268C166075782 @default.
• W2887375268 hasConceptScore W2887375268C171089720 @default.
• W2887375268 hasConceptScore W2887375268C181199279 @default.
• W2887375268 hasConceptScore W2887375268C185592680 @default.
• W2887375268 hasConceptScore W2887375268C207001950 @default.
• W2887375268 hasConceptScore W2887375268C2776317432 @default.
• W2887375268 hasConceptScore W2887375268C2777056448 @default.
• W2887375268 hasConceptScore W2887375268C2777180221 @default.
• W2887375268 hasConceptScore W2887375268C2780578515 @default.
• W2887375268 hasConceptScore W2887375268C2780841215 @default.
• W2887375268 hasConceptScore W2887375268C55493867 @default.
• W2887375268 hasConceptScore W2887375268C555293320 @default.
• W2887375268 hasConceptScore W2887375268C71924100 @default.
• W2887375268 hasConceptScore W2887375268C86803240 @default.
• W2887375268 hasFunder F4320321363 @default.
• W2887375268 hasLocation W28873752681 @default.
• W2887375268 hasLocation W28873752682 @default.
• W2887375268 hasOpenAccess W2887375268 @default.
• W2887375268 hasPrimaryLocation W28873752681 @default.
• W2887375268 hasRelatedWork W1975968177 @default.
• W2887375268 hasRelatedWork W1978718098 @default.
• W2887375268 hasRelatedWork W1985540243 @default.
• W2887375268 hasRelatedWork W1992423160 @default.
• W2887375268 hasRelatedWork W1999652479 @default.
• W2887375268 hasRelatedWork W2079804504 @default.
• W2887375268 hasRelatedWork W2092463003 @default.
• W2887375268 hasRelatedWork W3028691777 @default.
• W2887375268 hasRelatedWork W4220804802 @default.
• W2887375268 hasRelatedWork W2069423858 @default.
• W2887375268 hasVolume "835" @default.

• next