scholarly journals Microwave-assisted green synthesis of bile acid derivatives and evaluation of glucocorticoid receptor binding

2020 ◽  
Author(s):  
Bojana R. Vasiljević ◽  
Edward T. Petri ◽  
Sofija S. Bekić ◽  
Andjelka S. Ćelić ◽  
Ljubica M. Grbović ◽  
...  
Keyword(s):  
Bile Acid ◽  
Microwave Irradiation ◽  
Glucocorticoid Receptor ◽  
Ligand Binding ◽  
Green Synthesis ◽  
Bile Acids ◽  
Receptor Binding ◽  
Microwave Assisted ◽  
Bile Acid Derivatives ◽  
Cholanic Acid

Green synthesis of bile acids derivatives and 5β-cholanic acid was achieved under microwave irradiation, and the binding affinity for the ligand binding domain of the glucocorticoid receptor was measured.

Interaction between bile acids and staphylococcal polysaccharide: inhibition of capsule formation in encapsulated mutant strains (taurine+, taurine−) of Staphylococcus aureus

1983 ◽  
Vol 29 (12) ◽  
pp. 1653-1660 ◽  
Author(s):  
Toshichika Ohtomo
Keyword(s):  
Staphylococcus Aureus ◽  
Bile Acid ◽  
Bile Acids ◽  
Cholic Acid ◽  
Taurocholic Acid ◽  
Polysaccharide Antigen ◽  
Capsule Formation ◽  
Mutant Strains ◽  
Bile Acid Derivatives ◽  
Capsular Material

In a previous paper, we showed that bile acid derivatives inhibit capsule formation as well as taurine biosynthesis in a taurine+ (Tau+) encapsulated strain of Staphylococcus aureus. In the present study, binding of [14C]cholic acid ([14C]CA) and [14C]taurocholic acid ([14C]TA) to the staphylococcal polysaccharide antigen (SPA) of the capsular fraction was examined. The bile acids were found to bind with SPA via taurine of the Tau+ cells. [14C]CA bound with the SPA fraction of the Tau+ strain within 10–30 min, whereas 60–120 min was required in the binding of [14C]TA. Various bile acids competed with cholic acid binding to Tau+ cells which was shown by the inhibition of binding with cholic acid or taurocholic acid but not with glycholic acid. Binding of bile acid derivatives to a Tau− encapsulated mutant or to capsular material from this mutant was not observed.

scholarly journals Structural basis of bile acid receptor activation and Gs coupling

2020 ◽  
Author(s):  
Fan Yang ◽  
Chunyou Mao ◽  
Lulu Guo ◽  
Jingyu Lin ◽  
Qianqian Ming ◽  
...  
Keyword(s):  
Bile Acid ◽  
Ligand Binding ◽  
Bile Acids ◽  
G Protein ◽  
Binding Pocket ◽  
Receptor Activation ◽  
Structural Features ◽  
Ligand Binding Pocket ◽  
Bile Acid Receptor ◽  
Key Residues

AbstractG protein-coupled bile acid receptor (GPBAR) is a membrane receptor that senses bile acids to regulate diverse functions through Gs activation. Here, we report the cryo-EM structures of GPBAR–Gs complexes stabilized by either high-affinity P395 or the semisynthesized bile acid derivative INT-777 at 3-Å resolution. These structures revealed a large oval-shaped ligand pocket with several sporadic polar groups to accommodate the amphipathic cholic core of bile acids. A fingerprint of key residues recognizing diverse bile acids in the orthosteric site, a putative second bile acid binding site with allosteric properties and structural features contributing to bias property were identified through structural analysis and mutagenesis studies. Moreover, structural comparison of GPBAR with other GPCRs uncovered an atypical mode of receptor activation and G-protein– coupling, featuring a different set of key residues connecting the ligand binding pocket to the Gs coupling site, and a specific interaction motif localized in intracellular loop 3. Overall, our study not only provides unique structural features of GPBAR in bile acid recognition, allosteric effects and biased signaling, but also suggests that distinct allosteric connecting mechanisms between the ligand binding pocket and the G protein binding site exist in the GPCR superfamily.

scholarly journals Microwave irradiation: a green approach for the synthesis of functionalizedN-methyl-1,4-dihydropyridines

RSC Advances ◽  
2018 ◽  
Vol 8 (73) ◽  
pp. 41892-41903 ◽  
Author(s):  
M. Musawwer Khan ◽  
Saigal Saigal ◽  
Sarfaraz Khan ◽  
Sumbulunnisan Shareef ◽  
Subash C. Sahoo
Keyword(s):  
Microwave Irradiation ◽  
Green Synthesis ◽  
Microwave Assisted ◽  
Green Approach

Microwave-assisted green synthesis ofN-methyl-1,4-dihydropyridines under eco-friendly conditions.

scholarly journals Microwave-assisted, ligand-free, direct C–H arylation of thiophenes in biomass-derived γ-valerolactone

2017 ◽  
Vol 41 (17) ◽  
pp. 9210-9215 ◽  
Author(s):  
Silvia Tabasso ◽  
Emanuela Calcio Gaudino ◽  
Laura Rinaldi ◽  
Audrey Ledoux ◽  
Paolo Larini ◽  
...  
Keyword(s):  
Microwave Irradiation ◽  
Green Synthesis ◽  
Microwave Assisted ◽  
Ligand Free

We report a ligand-free green synthesis of arylthiophenes and poly(3-hexyl)thiophene in GVL under microwave irradiation.

Precipitation and 13C-NMR relaxation enhancement measurements of the interactions of bile acids with synthetic cationic bile acid derivatives, and with spin labelled fatty acids

1991 ◽  
Vol 60 (2) ◽  
pp. 143-151 ◽  
Author(s):  
David G. Reid ◽  
Kaushika Gajjar ◽  
Simon P. Robinson ◽  
Deirdre M.B. Hickey ◽  
G.Martin Benson ◽  
...  
Keyword(s):  
Fatty Acids ◽  
Bile Acid ◽  
Bile Acids ◽  
13C Nmr ◽  
Nmr Relaxation ◽  
Bile Acid Derivatives
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