Bile acids and their receptors in regulation of gut health and diseases

S Lin, S Wang, P Wang, C Tang, Z Wang… - Progress in Lipid …, 2023 - Elsevier
It is well established that bile acids play important roles in lipid metabolism. In recent
decades, bile acids have also been shown to function as signaling molecules via interacting …

The role of human 5-Lipoxygenase (5-LO) in carcinogenesis-a question of canonical and non-canonical functions

AS Kahnt, AK Häfner, D Steinhilber - Oncogene, 2024 - nature.com
Lipoxygenase (5-LO), a fatty acid oxygenase, is the central enzyme in leukotriene (LT)
biosynthesis, potent arachidonic acid-derived lipid mediators released by innate immune …

Chlorogenic acid attenuates inflammation in LPS-induced Human gingival fibroblasts via CysLT1R/Nrf2/NLRP3 signaling

X Huang, Y Liu, H Shen, T Fu, Y Guo, S Qiu - International …, 2022 - Elsevier
Periodontitis is a chronic periodontal inflammatory disease and its etiology remains not fully
understood. Chlorogenic acid (CA) is an ingredient isolated from nature product and exerts …

Combinatorial targeting of G‐protein‐coupled bile acid receptor 1 and cysteinyl leukotriene receptor 1 reveals a mechanistic role for bile acids and leukotrienes in …

M Biagioli, S Marchianò, C di Giorgio, R Roselli… - Hepatology, 2023 - journals.lww.com
Conclusions: By genetic and pharmacological approaches, we demonstrated that GPBAR1
and CYSLTR1 mutually interact in the development of DILI. A combinatorial approach …

[HTML][HTML] Microbial-derived bile acid reverses inflammation in IBD via GPBAR1 agonism and RORγt inverse agonism

M Biagioli, C Di Giorgio, C Massa, S Marchianò… - Biomedicine & …, 2024 - Elsevier
The interplay between the dysbiotic microbiota and bile acids is a critical determinant for
development of a dysregulated immune system in inflammatory bowel disease (IBD). Here …

Structural basis for developing multitarget compounds acting on cysteinyl leukotriene receptor 1 and G-protein-coupled bile acid receptor 1

B Fiorillo, V Sepe, P Conflitti, R Roselli… - Journal of Medicinal …, 2021 - ACS Publications
G-protein-coupled receptors (GPCRs) are the molecular target of 40% of marketed drugs
and the most investigated structures to develop novel therapeutics. Different members of the …

Discovery of a Potent and Orally Active Dual GPBAR1/CysLT1R Modulator for the Treatment of Metabolic Fatty Liver Disease

S Fiorucci, P Rapacciuolo, B Fiorillo… - Frontiers in …, 2022 - frontiersin.org
Nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH) are two
highly prevalent human diseases caused by excessive fat deposition in the liver. Although …

A microbial derived bile acid acts as GPBAR1 agonist and RORγt inverse agonist and reverses inflammation in inflammatory bowel disease

M Biagioli, C Di Giorgio, C Massa, S Marchiano'… - bioRxiv, 2024 - biorxiv.org
The interplay between the dysbiotic microbiota and bile acids is a critical determinant for
development of a dysregulated immune system in inflammatory bowel disease (IBD). Here …

[PDF][PDF] DOTTORATO IN SCIENZA DEL FARMACO XXXIII CICLO 2018/2020

PER LA SALUTE - fedoa.unina.it
Metabolic and inflammatory diseases, affecting the liver and gastrointestinal system, are
very widespread and often their pathogenesis is still unknown. Because these disorders …