Results 101 to 110 of about 49,196 (193)
Structure- and isoform-specific glucuronidation of six curcumin analogs
1. In the present study, we aimed to characterize the glucuronidation of six curcumin analogs (i.e. RAO-3, RAO-8, RAO-9, RAO-18, RAO-19, and RAO-23) derived from galangal using human liver microsomes (HLM) and twelve expressed UGT enzymes. 2.
Danyi Lu (842754) +4 more
core +1 more source
ABSTRACT Two‐dimensional (2D) monolayer cultures remain the workhorse of colorectal cancer (CRC) research and high‐throughput screening (HTS), yet they poorly recapitulate tissue architecture, extracellular matrix (ECM) cues, metabolic gradients, and multicellular heterogeneity that govern drug response in vivo. Over the past decade, three‐dimensional (
Sarah J. Harmych, Bhuminder Singh
wiley +1 more source
Ecopipam, a selective dopamine D1 receptor antagonist in development for Tourette syndrome, is primarily converted by uridine diphosphate‐glucuronosyltransferase (UGT)1A9 to ecopipam glucuronide, with a minor metabolic pathway by cytochrome P450 3A4 ...
Virginia D. Schmith +3 more
doaj +1 more source
The intestinal microbiome is a key regulator of immune homeostasis, metabolism, and epithelial barrier integrity. In patients with malignant hematological diseases, particularly those undergoing hematopoietic stem cell transplantation, microbiome perturbations by reduced diversity, pathobiont expansion, and loss of beneficial metabolites are common as ...
Bálint Gergely Szabó +7 more
wiley +1 more source
SGLT2i in heart failure: Cardiorenal mechanisms, clinical evidence and translational perspectives
SGLT2 inhibitors improve heart failure outcomes through integrated cardiorenal mechanisms. In the kidney, they reduce glucose and sodium reabsorption, promoting natriuresis, osmotic diuresis and renal protection. In the heart, they enhance myocardial energetics, reduce inflammation, oxidative stress, fibrosis and adverse remodelling, resulting in fewer
Jelica Grujic‐Milanovic +4 more
wiley +1 more source
Isoursodeoxycholic acid: metabolism and therapeutic effects in primary biliary cirrhosis1
Significant amounts of ursodeoxycholic acid (UDCA) used for the treatment of patients with primary biliary cirrhosis (PBC) become epimerized at C-3 to isoUDCA. We investigated the metabolism of isoUDCA and a possible pharmacologic effect in five patients
Hanns-Ulrich Marschall +5 more
doaj +1 more source
N-Glucuronidation of Drugs and Other Xenobiotics [PDF]
UDP-glucuronosyltransferases (UGTs) are a family of metabolic enzymes responsible for the detoxification of a wide range of endo- and xenobiotics, including drugs.
Kaivosaari, Sanna
core
Abstract Topiramate (TPM) is used to treat seizures in adults and children ≥2 years. In children, TPM dosing is body weight based. It is unknown whether children with obesity may benefit from an alternative dosing strategy. We developed a novel physiologically based pharmacokinetic (PBPK) model for TPM that accounts for age‐ and obesity‐related changes
Patricia D. Maglalang +14 more
wiley +1 more source
Mutual Regioselective Inhibition of Human UGT1A1-Mediated Glucuronidation of Four Flavonoids
UDP-glucuronosyltransferase (UGT) 1A1-catalyzed glucuronidation is an important elimination pathway of flavonoids, and mutually inhibitory interactions may occur when two or more flavonoids are coadministered.
Song Gao (131209) +5 more
core +1 more source
Fruquintinib: Mechanism of Action, Clinical, and Translational Science
ABSTRACT Fruquintinib is a highly selective, oral inhibitor of all three vascular endothelial growth factor receptors (‐1, ‐2, and ‐3) that was approved, including in China, the United States, and the European Union, for the treatment of previously treated metastatic colorectal cancer (mCRC).
Xiaofei Zhou +7 more
wiley +1 more source

