These comprise three members of the multidrug resistance family (MDR, gene ABCB) - the bile salt export pump (BSEP, gene ABCB11), MDR3 (ABCB4, Mdr2 in mouse) and MDR1 (ABCB1), as well as the MRP2 pump (gene ABCC
Another component in some of Unigene's oral formulations is the bile salt, sodium taurocholate [10,11]. Bile salts can routinely reach concentrations over 10 mm in the lumen in the fed state, which is high enough to both increase intestinal permeability and improve drug solubilisation [15]. ...
BA are actively secreted mainly by the bile salt export pump (BSEP; ABCB11/Abcb11) into the canaliculi [19] and then appear in bile, stored and concentrated in the gallbladder and periodically delivered to the intestine during fasting and mainly during the fat- cholecystokinin-dependent ...
BAs are conjugated to taurine or glycine mainly via two enzymes, BA CoA synthase (BACS) and BA-CoA-amino acid N-acetyltransferase (BAAT), secreted into bile by the bile salt export pump (BSEP); the multidrug resistance-associated protein (MRP2) mediates secretion of organic substrates such as...
On their side chain, BAs undergo deconjugation to form unconjugated BAs as well as free glycine or taurine residues (68). The enzymatic hydrolysis of the C-24 N-acyl amide bond, referred to as deconjugation, is catalyzed by bile salt hydrolase (BSH) enzymes in the small intestine, a proces...
Using a set 1.5 h program (37C_h_TDK_1cus) on the GentleMACS Octo Dissociator (Miltenyi Biotec), liver chunks were further digested by transferring 2-3 g of liver into gentleMACS C-tubes (Miltenyi Biotec) in 15 mL of Hanks’ Balanced Salt Solution (Sigma-Aldrich) with 1.2 Wünsch units...
formyl, acetyl, formamido, acetylamino, acetoxy, methylamino, dimethylamino, N-methylcarbamoyl, N,N-dimethylcarbamoyl, methylthio, methylsulphinyl, mesyl, N-methylsulphamoyl and N,N-dimethylsulphamoyl; or a pharmaceutically acceptable salt, solvate, solvate of such a salt or a prodrug thereof....
PFIC, type 2, which is sometimes referred to as “Byler syndrome,” is caused by impaired bile salt secretion due to mutations in the ABCB11 gene, which codes for a protein, known as the bile salt export pump, that moves bile acids out of the liver. Subjects with PFIC, type 2 often...
butyl-3-ethyl-7-(methylthio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)serine; and (R)—O—((S)-3-butyl-3-ethyl-7-(methylthio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)serine; or a pharmaceutically acceptable salt ...
-5-(4-fluorophenyl)-1,1-dioxido-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy)acrylic acid; (R)-(E)-3-((3-butyl-7-(ethylthio)-5-(4-fluorophenyl)-1,1-dioxido-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepin-8-yl)oxy)acrylic acid; or a pharmaceutically acceptable salt ...